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  • Synthesis, in‐vitro and in‐silico study of novel thiazoles as potent antibacterial agents and MurB inhibitors
    Arch. Pharm. (IF 2.145) Pub Date : 2020-01-22
    Sherif M. H. Sanad; Ahmed A. M. Ahmed; Ahmed E. M. Mekky
    更新日期:2020-01-23
  • Recent advances in isatin hybrids as potential anticancer agents
    Arch. Pharm. (IF 2.145) Pub Date : 2020-01-21
    Zhen Ding; Minfeng Zhou; Cheng Zeng
    更新日期:2020-01-22
  • 更新日期:2020-01-15
  • Synthesis and characterization of some new pyrazolines and their inhibitory potencies against carbonic anhydrases
    Arch. Pharm. (IF 2.145) Pub Date : 2020-01-10
    Gonca Çelik; Tayfun Arslan; Murat Şentürk; Deniz Ekinci
    更新日期:2020-01-11
  • rac‐ and meso‐Cyclohexanoids: Their α‐, β‐glycosidases, antibacterial, antifungal activities, and molecular docking studies
    Arch. Pharm. (IF 2.145) Pub Date : 2020-01-10
    Emel Karakılıç; Şule Baran; Hatice Öğütçü; Atilla Akdemir; Arif Baran
    更新日期:2020-01-11
  • Propafenone analogue with additional H‐bond acceptor group shows increased inhibitory activity on P‐glycoprotein
    Arch. Pharm. (IF 2.145) Pub Date : 2020-01-09
    Anna Cseke; Theresa Schwarz; Sankalp Jain; Simon Decker; Kerstin Vogl; Ernst Urban; Gerhard F. Ecker
    更新日期:2020-01-09
  • Design, synthesis, and biological evaluation of new 1,4‐diarylazetidin‐2‐one derivatives (β‐lactams) as selective cyclooxygenase‐2 inhibitors
    Arch. Pharm. (IF 2.145) Pub Date : 2020-01-09
    Hadi Arefi; Nima Naderi; Amir B. Irani Shemirani; Mina Kiani Falavarjani; Mahsa Azami Movahed; Afshin Zarghi
    更新日期:2020-01-09
  • Pharmacophore modeling, 3D‐QSAR, synthesis, and anti‐lung cancer evaluation of novel thieno[2,3‐d][1,2,3]triazines targeting EGFR
    Arch. Pharm. (IF 2.145) Pub Date : 2020-01-02
    Ranza Elrayess; Yasmine M. Abdel Aziz; Mohamed S. Elgawish; Marwa Elewa; Hosam A. Elshihawy; Mohamed M. Said
    更新日期:2020-01-02
  • Exploration of (3‐benzyl‐5‐hydroxyphenyl)carbamates as new antibacterial agents against Gram‐positive bacteria
    Arch. Pharm. (IF 2.145) Pub Date : 2020-01-02
    Hua‐ju Liang; Ya‐juan Cheng; Lu‐xia Wang; Bao‐qin Huang; Niu‐niu Zhang; Jie Liang; Ming Yan
    更新日期:2020-01-02
  • Synthesis and anti‐inflammatory effects of novel emodin derivatives bearing azole moieties
    Arch. Pharm. (IF 2.145) Pub Date : 2019-12-30
    Xiaokang Zhu; Qifang Chen; Yujin Yang; Xixi Ai; Si Chen; Yang Song
    更新日期:2019-12-30
  • Identification of novel selective Mtb‐DHFR inhibitors as antitubercular agents through structure‐based computational techniques
    Arch. Pharm. (IF 2.145) Pub Date : 2019-12-23
    Kalicharan Sharma; Nazia Neshat; Shweta Sharma; Namita Giri; Apeksha Srivastava; Faisal Almalki; Khalid Saifullah; Md. Mumtaz Alam; Mohammad Shaquiquzzaman; Mymoona Akhter
    更新日期:2019-12-23
  • Design, synthesis, antileishmanial, and antifungal biological evaluation of novel 3,5‐disubstituted isoxazole compounds based on 5‐nitrofuran scaffolds
    Arch. Pharm. (IF 2.145) Pub Date : 2019-12-16
    Ozildéia S. Trefzger; Natália V. Barbosa; Renata L. Scapolatempo; Amarith R. das Neves; Maria L. F. S. Ortale; Diego B. Carvalho; Antônio M. Honorato; Mariana R. Fragoso; Cristiane Y. K. Shuiguemoto; Renata T. Perdomo; Maria F. C. Matos; Marilene R. Chang; Carla C. P. Arruda; Adriano C. M. Baroni
    更新日期:2019-12-17
  • 更新日期:2019-12-06
  • Discovery of N‐pyridoyl‐Δ2‐pyrazolines as Hsp90 inhibitors
    Arch. Pharm. (IF 2.145) Pub Date : 2019-12-06
    Sundeep Kadasi, Ravali Yerroju, Swetha Gaddam, Nikhila Pullanagiri, Meghana Chary, Divya Pingili, Shiva Raj, Nulgumnalli Manjunathaiah Raghavendra
    更新日期:2019-12-06
  • 更新日期:2019-12-04
  • G protein‐coupled receptor binding and pharmacological evaluation of indole‐derived thiourea compounds
    Arch. Pharm. (IF 2.145) Pub Date : 2019-11-29
    Daniel Szulczyk, Anna Bielenica, Ewa Kędzierska, Anna Leśniak, Agata Pawłowska, Magdalena Bujalska‐Zadrożny, Irene Saccone, Rosa Sparaco, Ferdinando Fiorino, Oleksandra Savchenko, Marta Struga
    更新日期:2019-11-30
  • Synthesis, characterization, biological evaluation, and molecular docking studies of some piperonyl‐based 4‐thiazolidinone derivatives
    Arch. Pharm. (IF 2.145) Pub Date : 2019-11-28
    Hayriye Genc Bilgicli, Parham Taslimi, Busra Akyuz, Burak Tuzun, İlhami Gulcin
    更新日期:2019-11-29
  • New aryloxy‐quinone derivatives with promising activity on Trypanosoma cruzi
    Arch. Pharm. (IF 2.145) Pub Date : 2019-11-11
    Christian Espinosa‐Bustos, Karina Vázquez, Javier Varela, Hugo Cerecetto, Margot Paulino, Rodrigo Segura, Jaime Pizarro, Brenda Vera, Mercedes González, Ana M. Zarate, Cristian O. Salas
    更新日期:2019-11-11
  • Benzo[4,5]thieno[2,3‐d]pyrimidine phthalimide derivative, one of the rare noncompetitive inhibitors of dipeptidyl peptidase‐4
    Arch. Pharm. (IF 2.145) Pub Date : 2019-11-11
    Katarina Tomovic, Budimir S. Ilic, Marija Miljkovic, Stefan Dimov, Denitsa Yancheva, Milan Kojic, Anelia T. Mavrova, Gordana Kocic, Andrija Smelcerovic
    更新日期:2019-11-11
  • 1,2,4‐Triazole‐conjugated 1,3,4‐thiadiazole hybrid scaffolds: A potent ameliorant of carrageenan‐induced inflammation by lessening proinflammatory mediators
    Arch. Pharm. (IF 2.145) Pub Date : 2019-11-07
    Prateek Pathak, Parjanya K. Shukla, Vladislav Naumovich, Maria Grishina, Amita Verma, Vladimir Potemkin
    更新日期:2019-11-07
  • Synthesis, biological screening, and molecular docking of quinazolinone and quinazolinethione as phosphodiesterase 7 inhibitors
    Arch. Pharm. (IF 2.145) Pub Date : 2019-11-07
    Sherin M. Elfeky, Tariq R. Sobahi, Magdy M. Gineinah, Nesreen S. Ahmed
    更新日期:2019-11-07
  • Isatin–azole hybrids and their anticancer activities
    Arch. Pharm. (IF 2.145) Pub Date : 2019-11-06
    Yani Hou, Congshan Shang, Hui Wang, Jie Yun
    更新日期:2019-11-06
  • Structural Requirements of Histone Deacetylase Inhibitors: SAHA Analogs Modified on the Hydroxamic Acid.
    Arch. Pharm. (IF 2.145) Pub Date : 2016-04-12
    Anton V Bieliauskas,Sujith V W Weerasinghe,Ahmed T Negmeldin,Mary Kay H Pflum

    Histone deacetylase (HDAC) proteins have emerged as targets for anti-cancer therapeutics, with several inhibitors used in the clinic, including suberoylanilide hydroxamic acid (SAHA, vorinostat). Because SAHA and many other inhibitors target all or most of the 11 human HDAC proteins, the creation of selective inhibitors has been studied intensely. Recently, inhibitors selective for HDAC1 and HDAC2 were reported where selectivity was attributed to interactions between substituents on the metal binding moiety of the inhibitor and residues in the 14-Å internal cavity of the HDAC enzyme structure. Based on this earlier work, we synthesized and tested SAHA analogs with substituents on the hydroxamic acid metal binding moiety. The N-substituted SAHA analogs displayed reduced potency and solubility, but greater selectivity, compared to SAHA. Docking studies suggested that the N-substituent accesses the 14-Å internal cavity to impart preferential inhibition of HDAC1. These studies with N-substituted SAHA analogs are consistent with the strategy exploiting the 14-Å internal cavity of HDAC proteins to create HDAC1/2 selective inhibitors.

    更新日期:2019-11-01
  • 1,3-diaryl-2-propenones and 2-benzylidene-1,3-indandiones: a quest for compounds displaying greater toxicity to neoplasms than normal cells.
    Arch. Pharm. (IF 2.145) Pub Date : 2010-09-02
    Hari N Pati,Umashankar Das,Hiroshi Sakagami,Masame Kawase,Qing Chu,Qintao Wang,James P Stables,Jonathan R Dimmock

    A series of 1,3-diaryl-2-propenones 2a-j and analogous 2-benzylidene-1,3-indandiones 3a-j were evaluated against various neoplasms and normal cells. In general, greater cytotoxic potencies and selective toxicity to human malignant cells were observed by the compounds in series 2 rather than 3. In particular, 2i emerged as a lead molecule having an average CC(50) figure of 8.6 µM and a selective index value of 18. Various physicochemical features of 2a-j were correlated with the cytotoxic potencies to neoplastic cell lines which provide guidelines for expansion of this series of compounds. The enone 2i induced internucleosomal DNA fragmentation and activated caspase-3 in HL-60 cells suggesting that one of the ways in which the cytotoxicity of the compounds in series 2 is mediated towards some of the cell lines used in this study is by apoptosis. Neurotoxicity in mice was generally lower in series 2 than 3a-j.

    更新日期:2019-11-01
  • Mild synthetic approach to novel indole-1-carbinols and preliminary evaluation of their cytotoxicity in hepatocarcinoma cells.
    Arch. Pharm. (IF 2.145) Pub Date : 2012-06-21
    Gloria Zedda,Gabriella Simbula,Michela Begala,Monica Pibiri,Costantino Floris,Mariano Casu,Laura Casu,Graziella Tocco

    A mild and versatile method for the synthesis of some novel indole-1-carbinols has been developed via one-pot reaction of indoles and paraformaldehyde in the presence of an excess of CaO, MgO, ZnO or TiO(2). The solvent-free reaction provided all the indole derivatives in moderate to good yields and short reaction times. Moreover, the effect of some selected indole-1-carbinols on cell proliferation of the hepatoma cell line FaO was evaluated.

    更新日期:2019-11-01
  • Synthesis of imidazo[2,1-a]phthalazines, potential inhibitors of p38 MAP kinase. Prediction of binding affinities of protein ligands.
    Arch. Pharm. (IF 2.145) Pub Date : 2002-04-06
    Sylvie Mavel,Isabelle Thery,Alain Gueiffier

    Based upon molecular modeling, the pharmacophore of potential inhibitors of p38 MAPK (mitogen-activated protein kinases) is discussed and the predictive binding affinities are calculated. Syntheses of original diarylimidazo[2,1-a]phthalazines obtained by Suzuki coupling are described.

    更新日期:2019-11-01
  • Sigma receptor binding profile of a series of analgesic tropane derivatives.
    Arch. Pharm. (IF 2.145) Pub Date : 2002-04-06
    Orazio Prezzavento,Fulvio Gualtieri,Agostino Marrazzo,Maria Novella Romanelli,Giuseppe Ronsisvalle,Elisabetta Teodori

    The binding profile on sigma receptor subtypes of a family of tropane derivatives, previously studied as analgesic and nootropic drugs, is reported. The results show that the sigma receptors are not involved in the enhancement of acetylcholine release and of the consequent analgesic activity of this class of drugs. Structure-affinity relationships for sigma receptor subtypes are discussed. They lead to the identification of a few useful leads for further development of potent sigma ligands within the series.

    更新日期:2019-11-01
  • Synthesis and cytotoxicity of 9-alkoxy-1,5-dichloroanthracene derivatives in murine and human cultured tumor cells.
    Arch. Pharm. (IF 2.145) Pub Date : 2002-04-06
    Hsu-Shan Huang,Jeng-Fong Chiou,Hui-Fen Chiu,Rong-Fu Chen,Yu-Liang Lai

    9-Alkoxy-1,5-dichloroanthracenes were successfully prepared. Their cytotoxicity was evaluated in vitro on rat glioma C6 cell lines and human hepatoma G2 cell lines, respectively. Alkylation of 1,5-dichloro-9(10H)-anthracenone with either the appropriate alcohols or alkyl chlorides in the presence of sulfuric acid or sodium hydride, respectively, furnished this structural class of anthracenes. Contrary to mitoxantrone, cytotoxic properties were observed as documented by the reactivity of the novel compounds and potent in vitro activity against C6 cells and hep G2 cells over a wide range of structural variants. Among these compounds, 5c, 5h, 5l and 5n are potent cytotoxins. They inhibit C6 cell growth in culture, indicated by using 2,3-bis(2-methoxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilide sodium salt (XTT) colorimetric assay. By using this assay it was also shown that 5c, 5d and 5l possess potent cytotoxicity on hep G2 cells. The most active compound displaying in vitro cytotoxicity was the 9-butoxy derivative 5h with IC50 values 0.02 microM against C6 cells, as compared with mitoxantrone with IC50 values 0.07 microM. The most active compound displaying in vitro cytotoxicity against hep G2 cells was 5c with IC50 values 1.7 microM (mitoxantrone: 0.8 microM). Structure-activity relationships (SAR) of these compounds with respect to the nature of the alkoxy substitution in the 9 position are discussed for both cell lines.

    更新日期:2019-11-01
  • Benzo[1,2-c]1,2,5-oxadiazole N-oxide derivatives as potential antitrypanosomal drugs. Structure-activity relationships. Part II.
    Arch. Pharm. (IF 2.145) Pub Date : 2002-04-06
    Gabriela Aguirre,Hugo Cerecetto,Rossanna Di Maio,Mercedes González,Williams Porcal,Gustavo Seoane,Miguel A Ortega,Ignacio Aldana,Antonio Monge,Ana Denicola

    The preparation of new derivatives of benzo[1,2-c]1,2,5-oxadiazole N-oxide is described. These derivatives were chosen in order to investigate and confirm previous structural features found necessary to display an adequate antitrypanosomal activity. The compounds synthesized were tested in vitro against epimastigote forms of Trypanosoma cruzi. The presence of a bromine atom in the benzo system produced compounds less active than the corresponding de-halo analogues. However, 5-(bromomethyl)-7-bromobenzo[1,2-c]oxadiazole N-oxide (23) was the most cytotoxic compound against T. cruzi. For this, the 50% inhibitory dose (ID50) was determined, it was of the same order as that of Nifurtimox. From statistical analysis we could establish a relationship between lipophilic-hydrophilic balance of the derivatives with their effectiveness as antichagasic compounds.

    更新日期:2019-11-01
  • Synthesis and antimicrobial activities of 5-fluoro-1,2,6-trisubstituted benzimidazole carboxamide and acetamide derivatives.
    Arch. Pharm. (IF 2.145) Pub Date : 2002-02-02
    C Kus,H Göker,N Altanlar

    Some 5-fluoro-6-substitute-1 H-benzimidazole-2-carbamates (12a-e), 5-fluoro-6-substituted 1H-benzimidazole-2-acetate (13a-e) and 2-acetamide (14a-f) derivatives, 2-acetamido-5-fluoro-6-(morpholin-4-yl)-1-propyl-1H-benzimidazole (15), and 1-cyclopropyl-2-ethyl-5-fluoro-6-(4-methylpiperazin-1-yl)- 1H-benzimidazole (16) were synthesized, and their antimicrobial and antifungal activities evaluated. Compound 12c exhibited the best activity against Candida albicans.

    更新日期:2019-11-01
  • 1,4-dioxane-fused 4-anilinoquinazoline as inhibitors of epidermal growth factor receptor kinase.
    Arch. Pharm. (IF 2.145) Pub Date : 2002-02-02
    J Y Lee,Y K Park,S H Seo,I S So,H K Chung,B S Yang,S J Lee,H Park,Y S Lee

    The 4-anilinoquinazoline PD 153035 (1) is a potential antitumor agent which acts by inhibiting tyrosine kinase activity of epidermal growth factor receptor (EFGR) via competitive binding at the ATP site of enzyme. A series of cyclic analogues of PD 153035 bearing the 1,4-dioxane ring was prepared by reaction of 6-chloro derivative 5 with several aniline nucleophiles. These were evaluated for their ability to inhibit the EGFR kinase and the growth of primary human tumor cell cultures. All of the new 4-anilinoquinazolines exhibited less potency than PD 153035 against EGFR kinase. However, compounds 2b, 2c, 2e, 2g, and 2h showed higher inhibitory activities than PD 153035 against the growth of A431 tumor cell line. The compound 2b containing 3-chloroaniline ring was as potent as PD 153035 against EGFR kinase and showed about 5.4-fold better potency than PD153035 in the inhibition of growth of A431 cell line with good selectivity.

    更新日期:2019-11-01
  • Synthesis and biological investigations of 5-substituted pyrimidine nucleosides coupled to a dihydropyridine/pyridinium salt redox chemical delivery system.
    Arch. Pharm. (IF 2.145) Pub Date : 2002-02-02
    R Kumar,L Wang,L I Wiebe,E E Knaus

    The syntheses, antiviral activities, and partition coefficients (P) of 3'-O-(1-methyl-1,4-dihydropyridyl-3-carbonyl)-coupled nucleosides are described. These novel compounds were designed in an effort to enhance the lipophilicity, and thereby the delivery to the CNS, without compromising the anti-HSV-1 activity of the parental nucleosides. We have previously reported the synthesis of 3'-O-(1-methyl-1,4-dihydropyridyl-3- carbonyl) analogs of 5-iodo-(5), 5-vinyl-(6), and (E)-5-(2-iodovinyl)-2'-deoxyuridines (7). We now report the synthesis of 5-iodo-3'-O-(1-methyl-1,4-dihydropyridyl-3- carbonyl)-5'-O-acetyl-2'-deoxyuridine (15) and 3'-O-(1-methyl-1,4-dihydropyridyl-3-carbonyl)-2'-deoxyuridine (17). Quarternization of the 3'-O-(3-pyridylcarbonyl) compounds (10,12) using iodomethane afforded the corresponding 1-methyl pyridinium salts (13,14) which were reduced with sodium dithionite to yield the corresponding 3'-O-1-methyl-1,4-dihydropyridyl-3-carbonyl compounds (15,16). The deprotection of 3'-O-(1-methyl-1,4-dihydropyridyl- 3-carbonyl)-5'-O-t-butyldimethylsilyl-2'-deoxyuridine (16) with Bu4N+F- afforded 3'-O-(1-methyl-1,4-dihydropyridyl-3-carbonyl)-2'-deoxyuridine (17). Compounds 5-7 and 15 were evaluated for their antiviral activity in vitro against HSV-1, HSV-2, HCMV, and VZV, and were found to retain anti-HSV-1, HSV-2 and VZV activity as compared to their parental nucleosides (1-3). In addition, the cellular toxicity of 3'-O-(1-methyl-1,4-dihydropyridyl-3-carbonyl)-coupled compounds (5-7 and 15) was found to be lower than the parent nucleosides. The lipophilicity of compounds (5-7,15,17) are enhanced substantially, compared to the parent nucleosides, as indicated by an increase in corresponding P values (1-octanol-water) upon replacement of the C-3' hydroxyl by 1-methyl-1,4-dihydropyridyl-3-carbonyl moiety.

    更新日期:2019-11-01
  • Synthesis and biological properties of C-2, C-8, N-9 substituted 6-(3-chloroanilino)purine derivatives as cyclin-dependent kinase inhibitors. Part II.
    Arch. Pharm. (IF 2.145) Pub Date : 2002-02-02
    C H Oh,H K Kim,S C Lee,C Oh,B S Yang,H J Rhee,J H Cho

    In this study, C-2, C-8, N-9 substituted 6-(3-chloroanilino)purine derivatives were synthesized and their inhibitory effects on cyclin-dependent kinases (CDK2, 4) as well as their cytotoxicities were evaluated. The effects of substituents at the C-2, C-8, and N-9 positions of the substituted purine were investigated. Among the compounds tested, [6-(3-chloroanilino)-2-(2-hydroxymethyl-4-hydroxypyrrolidyl)-9- isopropylpurine] (4h) was the most active inhibitor of CDK2 with IC50 of 0.3 microM, i.e. a two-fold increased inhibitory activity as compared to roscovitine. Results from structure-activity relationship studies should allow the design of more potent and selective CDK2 inhibitors, which may provide an effective therapy for cancer or other CDK-dependant diseases.

    更新日期:2019-11-01
  • Synthesis and cytotoxicity of bis(benzo[g]indole-3-carboxamides) and related compounds.
    Arch. Pharm. (IF 2.145) Pub Date : 2002-02-02
    G A Pinna,M A Pirisi,G E Grella,L Gherardini,J M Mussinu,G Paglietti,A M Ferrari,G Rastelli

    A series of bis(benzo[g]indoles) bridged by CX-(CH2)nN(Me)(CH2)n-CX (X = O, S, H2; n = 2,3) was synthesized as bifunctional antitumor agents and evaluated for cytotoxic activity against diverse human cancer cell lines by the National Cancer Institute. The parent compounds 2a,b exhibited a good level of activity and derivates 2c-g,i,k demonstrated significant inhibitory effects, all with IC50 values in the low micromolar range. The thioamide analogue 2j showed less potency. It is interesting to note that introduction of substituents on the benzene ring of the benzo[g]indole portion of 2a,b did not affect activity, with the only exception of the 7,8-dichloro derivative 2h which became less potent. One member of this series, 2i, was then tested in the hollow fiber cell assay to evaluate, in a preliminary fashion, its in vivo antineoplastic activity. Molecular modelling studies were performed on amide 2a and thioamide 2j to explain the loss of activity of 2j as to 2a. Finally, compound 2a behaved as a typical DNA intercalating agent, as judged from viscosity measurements with Poly(dA-dT)...poly(dA-dT).

    更新日期:2019-11-01
  • Antinociceptive properties of chalcones. Structure-activity relationships.
    Arch. Pharm. (IF 2.145) Pub Date : 2002-01-05
    R Corrêa,M A Pereira,D Buffon,L dos Santos,V Cechinell Filho,A R Santos,R J Nunes

    Eleven chalcones were prepared and tested as antinociceptive agents using the writhing test in mice. Some compounds, given intraperitoneally, caused potent and dose-related antinociception, being several times more active than some reference drugs. The results evidenced that some physico-chemical parameters are involved in the pharmacological activity. 3,4-Dichlorochalcone (2) was the most effective compound, and was also studied in another model of pain in mice, the formalin test. Here it inhibited only the inflammatory pain (second phase), being equipotent to the reference drugs.

    更新日期:2019-11-01
  • Synthesis and anticonvulsant activity of N,N-phthaloyl derivatives of central nervous system inhibitory amino acids.
    Arch. Pharm. (IF 2.145) Pub Date : 2002-01-05
    C O Usifoh,D M Lambert,J Wouters,G K Scriba

    In order to study the influence of the length of the amino acid chain of N,N-phthaloyl-amino acid amides as analogues of the former anticonvulsant taltrimide on the seizure-antagonizing activity glycine, beta-alanine and gamma-aminobutyric acid (GABA) derivatives were synthesized. The corresponding taurine derivatives were also included. Generally, the glycine-derived amides showed a higher activity than the beta-alanine and GABA derivatives in the maximal electroshock seizure (MES) test in mice upon intraperitoneal administration. The activity was comparable to the respective taurine derivatives. The N,N-phthaloyl-glycine amides were also active in the MES test upon oral administration to rats. No significant activity was noted in the seizure threshold test with subcutaneous pentylene-tetrazole. The ED50 of N,N-phthaloyl-glycine ethyl amide (4b) in the MES test upon intraperitoneal administration to mice was 19.1 mg/kg. On a molar basis this activity is comparable to the activity of phenytoin with little toxicity in the rotorod test. In conclusion, N,N-phthaloyl-glycine amides might represent promising antiepileptic drugs.

    更新日期:2019-11-01
  • Naphthazarin derivatives (VIII): Synthesis, inhibitory effect on DNA topoisomerase-I, and antiproliferative activity of 6-(1-acyloxyalkyl)-5,8-dimethoxy-1,4-naphthoquinones.
    Arch. Pharm. (IF 2.145) Pub Date : 2002-01-05
    Y Kim,Y J You,B Z Ahn

    6-(1-Acyloxyalkyl)-5,8-dimethoxy-1,4-naphthoquinone (DMNQ; 5,8-dimethoxy-1,4-naphthoquinone) derivatives were synthesized and examined for their inhibitory effect on DNA topoisomerase-I (Topo I) and their antiproliferative activity against L1210 cells. The Topo-I inhibitory effect of 6-(1-hydroxyalkyl)-DMNQ derivatives was found to be dependent on the size of the alkyl chains, suggesting that lipophilicity might be one important factor influencing the inhibitory effect. It was found that acylation of 6-(1-hydroxyalkyl)-DMNQ derivatives possessing alkyl chains of C2-C5 enhanced both bioactivities, suggesting that an increase of electrophilicity in the quinoid moiety makes the electrophilic arylation of bionucleophiles more favorable. It is noteworthy that 6-(1-heptanoyloxyethyl)-DMNQ exhibited both the most potent Topo I inhibitory activity (IC50, 11.5 microM) and the greatest antiproliferative activity (ED50, 0.05 microM) upon L1210 cells.

    更新日期:2019-11-01
  • Does [meso-1,2-bis(2,6-dichloro-4-hydroxyphenyl)ethylenediamine] dichloroplatinum(II) act as an immune response modifier? IV. Inhibition of the proliferation-increasing effect of progressively growing MXT-M-3,2 breast cancer on phagocytes by the title compound.
    Arch. Pharm. (IF 2.145) Pub Date : 2002-01-05
    R Schlemmer,T Spruss,G Bernhardt,H Schönenberger

    In female B6D2F1 mice bearing an MXT-M-3,2 breast cancer graft the level of the phagocytic cells (e.g. of granulocytes and macrophages in the spleen and of granulocytes and monocytes in the blood) is significantly elevated. The positive correlation between the number of the phagocytic cells and the weight of the tumor indicates that the MXT-M-3,2 breast cancer promotes myelopoiesis, presumably by secretion of hematopoietic growth factors like GM-CSF. This process can be described for each phagocyte type by a regression equation. Due to its hormonal potency [meso-1,2-bis(2,6-dichloro-4-hydroxyphenyl)ethylenediamine] dichloroplatinum(II) (meso-1-PtCl2) can reduce the excessive numbers of the granulocytes and macrophages, which seem to be responsible for the progressive growth of the MXT-M-3,2 breast cancer. This process leads to an interruption of the vicious circle of mutual growth stimulation of breast cancer cells and these phagocytes. The target of meso-1-PtCl2 is the estrogen receptor (ER) of the breast cancer cell. The interaction between meso-1-PtCl2 and the ER presumably results in a diminished secretion of hematopoietic growth factors and hence in a decline of the number of phagocytic cells. Meso-1-PtCl2 does not inhibit the proliferation of tumor cells by direct interaction with their DNA, as is described for platinum complexes like cDDP. In its mode of action the equipotent, breast cancer inhibiting drug cDDP differs from meso-1-PtCl2. This is obvious from the fact that in cDDP--but not in meso-1-PtCl2-treated, tumor bearing mice the number of granulocytes and macrophages does not markedly deviate from that in untreated control mice with tumors of the same weight. The drug cDDP probably does not interfere with the mechanism of the secretion of hematopoietic growth factors. The reduction of the number of tumor cells by cDDP leads to a decline of the number of phagocytic cells in accordance with the respective regression equations. In contrast to meso-1-PtCl2 and cDDP, ovariectomy causes elevated phagocyte numbers, probably due to the strongly reduced estrogen level. The studies described in this publication indicate that the anti-breast cancer activity of meso-1-PtCl2 is caused by a decimation of phagocytes and with this by an abolition of the tumor promoting effect. Furthermore, a restoration of the natural immunosurveillance seems to be of importance.

    更新日期:2019-11-01
  • Synthesis and antifungal activity of 3,3'-ethylenebis(5-alkyl-1,3,5-thiadiazine-2-thiones).
    Arch. Pharm. (IF 2.145) Pub Date : 2002-01-05
    M A Hussein,A N El-Shorbagi,A R Khallil

    In a search for promising antifungal compounds, nine new 3,3'-ethylenebis(5-alkyl-1,3,5-thiadiazine-2-thiones) were synthesized by the reaction of ethylene diamine, carbon disulfide, formaldehyde, and the appropriate alkyl amine. The title compounds were tested for their antifungal activity in vitro against pathogenic (Trichophyton rubrum and Candida albicans), phytopathogenic (Penicillum expansum, Trichoderma hazianum, and Fasarium oxysporum), and aflatoxin producing (Aspergillus flavus) fungi. These compounds exhibited varied inhibitory effects on growth or sporulation of some tested fungal species.

    更新日期:2019-11-01
  • Conjoint molecules of cephalosporins and aminoglycosides.
    Arch. Pharm. (IF 2.145) Pub Date : 2001-11-02
    I Grapsas,S A Lerner,S Mobashery

    A general synthetic route to conjoint molecules of cephalosporins and aminoglycosides is described. These molecules were designed as potential substrates for bacterial beta-lactamases, enzymes that hydrolyze the beta-lactam bond of cephalosporins. Hydrolysis of the beta-lactam bond was expected to release the C10-appended aminoglycoside. Since beta-lactamases are sequestered in the periplasmic space of gram-negative bacteria, this sequence of events would liberate aminoglycoside inside such bacteria. It is expected that such local delivery of aminoglycosides would circumvent the inherent toxicity of aminoglycosides that occurs during systemic exposure within the mammalian host.

    更新日期:2019-11-01
  • Synthesis, in vitro metabolic studies, and antitumour activity of methyl analogues of ifosfamide.
    Arch. Pharm. (IF 2.145) Pub Date : 2001-11-02
    K Misiura,K Kardacka,H Kusnierczyk

    Synthesis of 2-chloro-1,1-dimethylethyl and 2-chloro-2,2-dimethylethyl analogues of ifosfamide was performed via aziridine intermediate. In vitro metabolic activation showed that both compounds are metabolised at a rate similar to the parent drug. However, their anticancer activity against L1210 leukaemia in mice was lower as compared with ifosfamide. The reduction of antitumour efficiency of examined analogues is probably caused by a lower ability to cross-link DNA by their final, active metabolites.

    更新日期:2019-11-01
  • Synthesis and opioid-receptor binding of novel amino-substituted morphan analogues.
    Arch. Pharm. (IF 2.145) Pub Date : 2001-11-02
    G Höfner,B Streicher,B Wünsch

    Starting with methyl 4,6-O-benzylidene-alpha-D-glucopyranoside (4), an optimized procedure is reported for preparation of the bromide 7, which is transformed into the N-acylated heptopyranosamine 9. After introduction of an axially positioned azido moiety in position 3 intramolecular N/O-acetal formation succeeds to provide the morphan analogue 17. In receptor binding studies with radioligands the amines 18b-18d reveal higher affinity for mu-receptors than for kappa-receptors. The most mu-active compound 18b (Ki = 14 nM) contains two aryl substituents, which presumably may occupy both aryl binding sites of mu-receptors.

    更新日期:2019-11-01
  • Synthesis and antinociceptive activity of [(2-oxobenzothiazolin-3-yl)methyl]-4-alkyl/aryl-1,2,4-triazoline-5-thiones.
    Arch. Pharm. (IF 2.145) Pub Date : 2001-11-02
    M Gökce,B Cakir,K Erol,M F Sahin

    The synthesis and pharmacological evaluation of new [(2-oxobenzothiazolin-3-yl)methyl]-4-alkyl/aryl-1,2,4-triazoline-5-thiones are reported. All compounds were screened for analgesic and antiinflammatory activities by using the AcOH induced-stretching test, the hot plate test, the tail clip test, and the tail flick test. All of the title compounds showed more potent activity than the standard compound aspirin in the AcOH induced-stretching test. In the hot plate test [(2-oxobenzothiazolin-3-yl)methyl]-4-phenethyl-1,2,4-triazoline-5-thione 5j were revealed to be two-fold more potent in antinociceptive activity than novalgine. However, in the tail flick and tail clip test none of the compounds showed an antinociceptive activity as high as that of novalgine. On the basis of available data the structure-activity relationship in the [(2-oxobenzothiazolin-3-yl)methyl]-4-alkyl/aryl-1,2,4-triazoline-5-thiones was also discussed.

    更新日期:2019-11-01
  • 2'-substituted analogs of cocaine: synthesis and dopamine transporter binding potencies.
    Arch. Pharm. (IF 2.145) Pub Date : 2001-11-02
    T F el-Moselhy,K S Avor,G P Basmadjian

    A series of 2'-substituted cocaine analogs (4-8) was prepared and evaluated in an in vitro dopamine transporter (DAT) binding assay. Compounds 4-7 were prepared by esterifying the 3 beta-hydroxyl group of ecgonine methyl ester (3) using the appropriate acid chloride in the presence of Et3N and benzene. Compound 3 was obtained from cocaine (1) by hydrolysis using 1N HCl to afford ecgonine.HCl which was subjected to acid catalyzed esterification using methanol saturated with HCl gas. Compound 8 was obtained by hydrogenation of 7 using H2/Pd-C. The IC50 values were calculated from displacement experiment of the radioligand [3H]WIN-35,428 (2). 2'-Aminococaine (8) showed high binding affinity to the DAT (14- and 1.3-fold more active than cocaine and the radioligand 2, respectively). These results, along with previous results, emphasize the importance of a hydrogen-bond donor group at the 2'-position of cocaine to enhance binding affinity to the DAT.

    更新日期:2019-11-01
  • Ellipticine analogues and related compounds as inhibitors of reverse transcriptase and as inhibitors of the efflux pump.
    Arch. Pharm. (IF 2.145) Pub Date : 2001-11-02
    D Sharples,G Hajós,Z Riedl,D Csányi,J Molnár,D Szabó

    Ten polycyclic derivatives related to ellipticine have been synthesised and tested for their intercalating, reverse transcriptase (RT) inhibitory and multidrug resistance efflux pump inhibitory properties. The intercalating activity and the RT inhibitory activity of the derivatives suggest that ellipticine analogues bind at an allosteric binding site on RT or that this inhibition could be controlled at the DNA level. The MDR efflux pump inhibitory activities of these derivatives, however, appears to be unrelated to the DNA binding ability.

    更新日期:2019-11-01
  • Sydnone derivatives. Part VII: Synthesis of some novel thiazoles and their pharmacological properties.
    Arch. Pharm. (IF 2.145) Pub Date : 2001-11-02
    B Kalluraya,A M Rahiman,D Banji

    The synthesis of some 4-(arylsydnonyl)-2-(4-arylhydrazono-3-methyl-5-oxo-2-pyrazolin-1-yl)- thiazoles by reacting 1-thiocarboxamido-3-methyl-4-(aryihydrazono)-2-pyrazolin-5-ones with different 4-bromoacetyl-3-arylsydnones is described. A few compounds from this series were screened for their anti-inflammatory, analgesic, and CNS depressant activities. Among the tested compounds 6s, 6d, 6n, and 6u showed significant anti-inflammatory activity comparable with that of standard drug Ibuprofen. Compounds containing chlorine and carboxylic substituents are more active. 6f, 6r, and 6u showed marked analgesic activity and most of the compounds tested showed promising CNS depressant activity comparable with that of standard drug pentobarbitone.

    更新日期:2019-11-01
  • A comparative study of the enantiomeric resolution of several tetralone derivatives on macrocyclic antibiotic chiral stationary phases using HPLC under normal phase mode.
    Arch. Pharm. (IF 2.145) Pub Date : 2001-08-22
    H Y Aboul-Enein,I Ali

    The enantiomeric resolution of five substituted 2-(4-pyridylalkyl)-1-tetralone derivatives has been achieved on three macrocyclic glycopeptide antibiotic chiral stationary phases namely, Chirobiotic R, T, and V columns. The mobile phase used was hexane-ethanol-triethylamine (12:8:0.01, v/v/v). The flow rates were 1 mL/min for Chirobiotic T and 2 mL/min for Chirobiotic R and V respectively. The UV detection was carried out at 254 nm. The values of alpha of the resolved enantiomers of the reported tetralone derivatives were in the range of 1.32 to 2.51 on Chirobiotic R, 2.02 to 2.88 on Chirobiotic T and 1.55 to 2.54 on Chirobiotic V respectively while the values of Rs were in the range of 1.00 to 2.50 on Chirobiotic R, 1.00 to 1.95 on Chirobiotic T and 1.00 to 1.60 on Chirobiotic V respectively. The best resolution was achieved on Chirobiotic R column.

    更新日期:2019-11-01
  • Two sulfonamides-containing dihydropyrone derivatives as HIV protease inhibitors.
    Arch. Pharm. (IF 2.145) Pub Date : 2001-08-22
    J Y Lee,S N Kim,C K Lee,H Park,Y S Lee

    更新日期:2019-11-01
  • A simple procedure for synthesis of roxindole, a dopamine D2-receptor agonist.
    Arch. Pharm. (IF 2.145) Pub Date : 2001-08-22
    F Csende

    A modified convenient and high yielding synthetic route for the preparation of the dopamine agonist roxindole 1 is described. The key step in our method is the phase-transfer catalyzed reaction of gamma-butyrolactone with 5-methoxyindole which results in the indolylbutyric acid derivative directly in one step.

    更新日期:2019-11-01
  • Improvement and validation of the fluorescence-based histone deacetylase assay using an internal standard.
    Arch. Pharm. (IF 2.145) Pub Date : 2001-08-22
    K Hoffmann,B Heltweg,M Jung

    The determination of the activity of histone deacetylase (HDAC) and the potency of its inhibitors has become an important goal in medicinal chemistry. This is due both to the involvement of HDAC in gene regulation and the ability of its inhibitors to modulate transcription and induce differentiation and/or apoptosis in cancer cells. We have previously reported the development of a non-isotopic assay for HDAC using a fluorescent derivative of epsilon-acetyl lysine. It can replace existing methods that rely on radioactively labeled histones or oligopeptides as substrates. Here we report validation and improvement of the procedure using an internal standard for the quantitation of the fluorescent substrate by HPLC.

    更新日期:2019-11-01
  • Synthesis and 5-HT2A antagonist activity of derivatives of the novel heterocycles indolo[3,2-d]pyrrolo[3,2-g]azecine and benzo[d]pyrrolo[3,2-g]azecine compared to the benz[d]indolo[2,3-g]azecine derivative LE 300.
    Arch. Pharm. (IF 2.145) Pub Date : 2001-08-22
    S A Rostom,A M Farghaly,F S Soliman,M M el-Semary,S Elz,J Lehmann

    An indolo[3,2-d]pyrrolo[3,2-g]azecine and a benzo[d]pyrrolo[3,2-g]azecine analogue of the potent dopamine receptor antagonist LE 300 (7-methyl-6,7,8,9,14,15-hexahydro-5H-benz[d]indolo[2,3-g]azecine) have been prepared in multi-step reactions via C-N bond cleavage of corresponding quaternary N-methylquinolizinium iodides. LE 300, the target compounds and two precursor quinolizines have been tested in vitro for antagonist activity at 5-HT2A receptors (rat tail artery) and H1 receptors (guinea-pig ileum), respectively. LE 300 and compound 19 (3,6-dimethyl-4,5,6,7,8,13-hexahydro-3H-benzo[d]pyrrolo[3,2-g]azecine) competitively inhibited 5-HT-induced contractions with similar nanomolar potency (pA2 = 8.32 and 8.01, respectively) but were less active than the reference antagonist ketanserin (pA2 = 9.55). Compound 19 displayed moderate H1-antihistaminic activity in the guinea-pig ileum assay (pA2 = 7.37).

    更新日期:2019-11-01
  • Aromatic extended bisamidines: synthesis, inhibition of topoisomerases, and anticancer cytotoxicity in vitro.
    Arch. Pharm. (IF 2.145) Pub Date : 2001-08-22
    K Bielawski,A Bielawska,S Wołczyński

    A series of four aromatic extended bisamidines (12-15) differing in the nature of their terminal basic side chains were synthesized and evaluated for cytotoxic activity in MCF-7 cultured breast cancer cells. The concentrations of 12, 13, 14, and 15 needed to inhibit [3H]thymidine incorporation into DNA by 50% (IC50) were found to be 63 microM, 85 microM, 77 microM, and 97 microM, respectively. To test whether cytotoxic properties were related to DNA-binding and topoisomerase action, the bisamidines 12-15 were evaluated in a cell-free system. Data from the ethidium displacement assay showed that bisamidines 12-15 have significant affinity for DNA and show moderate specificity for AT base pairs. In the topoisomerase II assay, the relaxation of DNA was inhibited with all four drugs and the extent of inhibition was directly proportional to the drug concentration. This suggests that DNA binding may be implicated in the cytotoxicity of these bisamidines, possibly by inhibiting interactions between topoisomerase II and their DNA targets.

    更新日期:2019-11-01
  • Targeting of human Tmolt4 leukemic type II IMP dehydrogenase by cyclic imide related derivatives.
    Arch. Pharm. (IF 2.145) Pub Date : 2001-08-22
    I H Hall,B J Barnes,E S Ward,J R Wheaton,K A Shaffer,S E Cho,A E Warren

    2,3-Dihydrophthalazine-1,4-diones, indazolones, 3-imino-1-oxoisodolines, homophthalimides, napthalidimides, diphenamides, and 6,7-dihydro-5H-dibenz[c,e]azepines proved to be potent inhibitors of the activity of human Tmolt4 T cell leukemia Type II IMP dehydrogenase (IMPDH). This inhibition was competitive, yielding Ki values in the range of 1.96 to 48.9 microM. The inhibition of Type II IMPDH correlated positively with the inhibition of the growth of Tmolt4 cells, the syntheses of DNA and purine, and the activity of crude IMPDH. The Type II IMPDH isoform is found in rapidly proliferating cells. The isoform present in normal resting cells, Type I IMPDH, was elevated by the compounds at 100 microM. In addition, Compound 5 significantly increased the Type I enzyme activity in a concentration and time dependent manner. The selectivity of these derivatives towards Type II IMPDH will allow for the separation of cellular effects, which should reduce clinical toxicity when treating with antimetabolite IMPDH inhibitors.

    更新日期:2019-11-01
  • Synthesis of 3-nitrosoimidazo[1,2-a]pyridine derivatives as potential antiretroviral agents.
    Arch. Pharm. (IF 2.145) Pub Date : 2001-08-22
    A Chaouni-Benabdallah,C Galtier,H Allouchi,A Kherbeche,J C Debouzy,J C Teulade,O Chavignon,M Witvrouw,C Pannecouque,J Balzarini,E de Clercq,C Enguehard,A Gueiffier

    Ten 2-aryl or heteroaryl-3-nitrosoimidazo[1,2-a]pyridine derivatives were synthesised as potential antiretroviral agents. The new compounds were characterized by elemental analysis, 1H NMR, and by crystallography for (14). The compounds were devoid of any activity against HIV-1 or HIV-2.

    更新日期:2019-11-01
  • Synthesis and antiproliferative activity in vitro of new derivatives of 3-aminopyrazolo[3,4-b]pyridine. Part 1. Reaction of 3-aminopyrazolo[3,4-b]pyridine with 1,3-, 1,4-diketones and alpha,beta-unsaturated ketones.
    Arch. Pharm. (IF 2.145) Pub Date : 2001-08-22
    K Poreba,A Opolski,J Wietrzyk,M Kowalska

    The synthesis of several new pyrazolo[3,4-b]pyridine, pyrido[2',3':3,4]-pyrazolo[1,5-a]pyrimidine and imidazo[1',2':1,5]pyrazolo[3,4-b]pyridine derivatives is described. The obtained compounds were tested for their antiproliferative activity in vitro. One of them, 4-phenyl-2-(3,4,5-trimethoxy-beta-styrylo)pyrido- [2',3':3,4]pyrazolo[1,5-a]pyrimidine (9), revealed cytotoxic properties against the cells of all three human cancer cell lines applied. Another one, 2,4-dimethyl-pyrido[2',3':3,4]pyrazolo[1,5-a]-pyrimidine (2), revealed weak cytotoxic activity only against the cells of human bladder cancer cell line HCV29T. All other compounds tested did not reveal any cytotoxic activity.

    更新日期:2019-11-01
  • Coumarin derivatives as protease-sensitive prodrugs.
    Arch. Pharm. (IF 2.145) Pub Date : 2001-07-31
    K Achilles

    To overcome the lack of selectivity of anticancer drugs toward malignant cells, the development of prodrugs, which could be activated selectively by tumour-specific proteases is the goal of these studies. In this work tripartate prodrugs have been evaluated consisting of a carrier unit and a spacer group, which allows for intramolecular cyclisation while releasing the third component, the compound attached to the carboxylic acid moiety of the spacer group. As carrier units amino acids or peptides have been used, which are required for recognition by the protease. As the spacer unit the "trimethyl-lock"-spacer has been applied; as a model leaving group p-anisidine was attached to the carboxylic acid moiety. It was intended to test the compounds for their releasing rate of p-anisidine. Two of the evaluated compounds, 9b and 9h, were degraded with half-lives of 46 min at room temperature. However, the poor solubility in aqueous solutions proved the major disadvantage of the TML-based prodrugs.

    更新日期:2019-11-01
  • Synthesis and antitumour activity of 1H,3H-thiazolo[3,4-a]benzimidazole derivatives.
    Arch. Pharm. (IF 2.145) Pub Date : 2001-07-31
    A Chimirri,P Monforte,L Musumeci,A Rao,M Zappalà,A M Monforte

    A series of 1H,3H-thiazolo[3,4-a]benzimidazoles were synthesized and tested for their in vitro antitumour activity against 60 human tumour cell lines. Some derivatives exhibited both tumour growth inhibition activity and cellular selectivity. In particular, compound 8c, the most active of the series, was very active towards all cell lines at concentrations ranging from 10(-7)-10(-5) M. Compound 4a, on the other hand, was highly selective against the CNS cancer cell line.

    更新日期:2019-11-01
  • Inactivation of protein farnesyltransferase by active-site-targeted dicarbonyl compounds.
    Arch. Pharm. (IF 2.145) Pub Date : 2001-07-31
    K J Okolotowicz,W J Lee,R F Hartman,A Y Kim,S R Ottersberg,D E Robinson,S R Lefler,S D Rose

    Upon farnesylation by protein farnesyltransferase (FTase), key proteins become compartmentalized in cells. For example, cell membrane localization is essential for the mitogenic role of mutant Ras protein, which acts as a switch for cancer cell proliferation. We report that alpha-dicarbonyl compounds derived from the isoprenoid skeleton or other hydrophobic groups potently obstruct farnesylation of a Ras model peptide by human recombinant FTase in vitro. A geranyl-derived isoprenoid diketone, 5,9-dimethyl-8-decene-2,3-dione, at 17 microM caused a 62% reduction in FTase activity after 30 minutes. A farnesyl-derived isoprenoid diketone, 5,9,13-trimethyl-8,12-tetradecadiene-2,3-dione, at 93 microM caused a 94% reduction after 30 minutes. Other dicarbonyl compounds found to be effective against FTase in vitro were (+/-)-6-(camphorquinone-10-sulfonamido)-hexanoic acid, 4,4'-biphenyldiglyoxaldehyde, dehydroascorbic acid 6-palmitate, 2-oxododecanal, and phenylglyoxal. Higher concentrations of the alpha-dicarbonyl compound resulted in more rapid and more extensive inactivation. These findings demonstrate that alpha-dicarbonyl compounds targeted to FTase interfere with protein farnesylation in vitro and may lead to derivatives that have utility as chemotherapeutic agents.

    更新日期:2019-11-01
  • Potential tuberculostatic agents: micelle-forming copolymer poly(ethylene glycol)-poly(aspartic acid) prodrug with isoniazid.
    Arch. Pharm. (IF 2.145) Pub Date : 2001-07-31
    M Silva,A S Lara,C Q Leite,E I Ferreira

    With the objective of obtaining slow-acting isoniazid derivatives, of potential use as chemoprophylactics or chemotherapeutics in tuberculosis, the micelle-forming copolymer of poly(ethylene glycol)-poly(aspartic acid) prodrug with isoniazid was synthesized. The derivative obtained was found to be active in Mycobacterium tuberculosis culture, with a minimal inhibitory concentration (MIC) 5.6 times lower than that of the tuberculostatic drug.

    更新日期:2019-11-01
  • 1-Pyrrolines (3,4-dihydro-2H-pyrroles) as a template for new drugs.
    Arch. Pharm. (IF 2.145) Pub Date : 2001-07-31
    G Dannhardt,W Kiefer

    更新日期:2019-11-01
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