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Editorial: Professor Gerhard Klebe's 70th birthday and lifetime achievements in drug design Arch. Pharm. (IF 5.1) Pub Date : 2024-04-22 Hans‐Joachim Böhm
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Spectroscopic investigation and structural simulation in human serum albumin with hydroxychloroquine/Silybum marianum and a possible potential COVID‐19 drug candidate Arch. Pharm. (IF 5.1) Pub Date : 2024-04-22 Maryam S. H. Tekyeh, Seyed M. M. Shushtarian, Alireza I. Bakhsh, Saeed H. Tackallou, Hossein Lanjanian
In this study, the interaction between human serum albumin (HSA) and the hydroxychloroquine/Silybum marianum (HCQ/SM) mixture was investigated using various techniques. The observed high binding constant (Kb) and Stern–Volmer quenching constant (KSV) indicate a strong binding affinity between the HCQ/SM mixture and HSA. The circular dichroism (CD) analysis revealed that HCQ/SM induced conformational
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Novel RP‐HPLC method for estimation of a newly developed combination of tizanidine and etoricoxib in rat plasma: Eight criteria for greens evaluation Arch. Pharm. (IF 5.1) Pub Date : 2024-04-22 Eman A. Assirey, Hoda A. Ahmed, Rawan AL‐Faze, M. S. Amin, Samar M. Mahgoub, Fatma I. Abo El‐Ela, Mahmoud A. Mohamed
A novel environmentally friendly reversed‐phase high‐performance liquid chromatography (RP‐HPLC) method has been effectively validated for simultaneously measuring a prospective conjunction of tizanidine (TIZ) and etoricoxib (ETC), the combined medicine, in rat plasma. The technique employs diclofenac potassium as the internal standard, guaranteeing dependable and precise outcomes. This study aimed
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Assessment of fragment docking and scoring with the endothiapepsin model system Arch. Pharm. (IF 5.1) Pub Date : 2024-04-17 Carina Herbst, Sara Endres, Rebecca Würz, Christoph Sotriffer
Fragment‐based screening has become indispensable in drug discovery. Yet, the weak binding affinities of these small molecules still represent a challenge for the reliable detection of fragment hits. The extent of this issue was illustrated in the literature for the aspartic protease endothiapepsin: When seven biochemical and biophysical in vitro screening methods were applied to screen a library of
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New 2‐nitroimidazole‐N‐acylhydrazones, analogs of benznidazole, as anti‐Trypanosoma cruzi agents Arch. Pharm. (IF 5.1) Pub Date : 2024-04-17 Marcelly C. S. R. Pitombeira, Policarpo A. S. Júnior, Silvane Maria Fonseca Murta, Alvaro Romanha, Pedro H. Luccas, M. Cristina Nonato, Rafael E. O. Rocha, Rafaela S. Ferreira, Flávia F. da Silveira, Frederico S. Castelo‐Branco, Alcione S. Carvalho, Nubia Boechat
Chagas disease is a neglected tropical parasitic disease caused by the protozoan Trypanosoma cruzi. Worldwide, an estimated 8 million people are infected with T. cruzi, causing more than 10,000 deaths per year. Currently, only two drugs, nifurtimox and benznidazole (BNZ), are approved for its treatment. However, both are ineffective during the chronic phase, show toxicity, and produce serious side
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Spirooxadiazoline‐oxindoles derived from imatinib show antimyeloproliferative potential in K562 cells Arch. Pharm. (IF 5.1) Pub Date : 2024-04-17 Liviane D. de Azevedo, Debora I. Leite, Andressa P. de Oliveira, Floriano P. S. Junior, Rafael F. Dantas, Monica M. Bastos, Nubia Boechat, Luiz C. F. Pimentel
Imatinib mesylate was the first representative BCR‐ABL1 tyrosine kinase inhibitor (TKI) class for the treatment of chronic myeloid leukemia. Despite the revolution promoted by TKIs in the treatment of this pathology, a resistance mechanism occurs against all BCR‐ABL1 inhibitors, necessitating a constant search for new therapeutic options. To develop new antimyeloproliferative substances, we applied
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What doesn't fit is made to fit: Pim‐1 kinase adapts to the configuration of stilbene‐based inhibitors Arch. Pharm. (IF 5.1) Pub Date : 2024-04-17 Phil M. M. Hochban, Lukas Heyder, Andreas Heine, Wibke E. Diederich
Recently, we have developed novel Pim‐1 kinase inhibitors starting from a dihydrobenzofuran core structure using a computational approach. Here, we report the design and synthesis of stilbene‐based Pim‐1 kinase inhibitors obtained by formal elimination of the dihydrofuran ring. These inhibitors of the first design cycle, which were obtained as inseparable cis/trans mixtures, showed affinities in the
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Metabolic profiling of Verbena bonariensis L. extract by LC/MS and evaluation of the hepatoprotective potential with isoniazid‐ and rifampicin‐induced hepatotoxicity in rats Arch. Pharm. (IF 5.1) Pub Date : 2024-04-12 Saiqa Ishtiaq, Saira Rehman, Sairah Hafeez Kamran, Zahid Mehmood Akhtar, Mai Albaik, Sameh S. Elhady
The study explored the hepatoprotective activity and metabolic profile of Verbena bonariensis L. methanol extract (VBM) and fractions using isoniazid as well as rifampicin‐triggered liver toxicity in Wistar albino rats. Metabolite profiling of VBM using HPLC‐PDA‐ESI‐MS identified 12 compounds, mainly iridoids, phenylpropanoids, and flavonoids, where verbascoside represents the major compound. Different
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New phenylthiosemicarbazide‐phenoxy‐1,2,3‐triazole‐N‐phenylacetamides as dual inhibitors against α‐glucosidase and PTP‐1B for the treatment of type 2 diabetes Arch. Pharm. (IF 5.1) Pub Date : 2024-04-09 Shirin Ansariashlaghi, Azadeh Fakhrioliaei, Maryam Mohammadi‐Khanaposhtani, Milad Noori, Mehdi Asadi, Somayeh Mojtabavi, Mohammad A. Faramarzi, Ensieh N. Esfahani, Hossein Rastegar, Bagher Larijani, Homa Azizian, Mohammad Mahdavi
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Novel 2‐[thio]acetamide linked quinazoline/1,2,4‐triazole/chalcone hybrids: Design, synthesis, and anticancer activity as EGFR inhibitors and apoptotic inducers Arch. Pharm. (IF 5.1) Pub Date : 2024-04-09 Ahmed S. Abdelkhalek, Hend Kothayer, Mostafa K. Soltan, Samy M. Ibrahim, Samar S. Elbaramawi
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Piperlongumine and its derivatives against cancer: A recent update and future prospective Arch. Pharm. (IF 5.1) Pub Date : 2024-04-09 Shasank S. Swain, Sanjeeb K. Sahoo
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Efficient, rapid, and high‐yield synthesis of aryl Schiff base derivatives and their in vitro and in silico inhibition studies of hCA I, hCA II, AChE, and BuChE Arch. Pharm. (IF 5.1) Pub Date : 2024-04-09 Musa Özil, Halis T. Balaydın, Berna Dogan, Murat Şentürk, Serdar Durdagi
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Novel multifunctional tacrine–donepezil hybrids against Alzheimer's disease: Design synthesis and bioactivity studies Arch. Pharm. (IF 5.1) Pub Date : 2024-04-09 Gülşah Bayraktar, Manuela Bartolini, Maria Laura Bolognesi, Mumin Alper Erdoğan, Güliz Armağan, Ece Bayır, Aylin Şendemir, Donatella Bagetta, Stefano Alcaro, Vildan Alptüzün
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Synthesis, characterization, and biological study of new synthetic opioid hemorphin‐4 peptides containing sterically restricted nonnatural amino acids Arch. Pharm. (IF 5.1) Pub Date : 2024-04-05 Petar Todorov, Stela Georgieva, Claudio Trapella, Kalin Chakarov, Jana Tchekalarova, Daniela Pechlivanova, Diana Cheshmedzhieva, Anna Fantinati, Davide Illuminati
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New enantioenriched β‐indolyl ketones as aromatase inhibitors: Unraveling heme–ligand interactions by MD simulation and MMPBSA analysis Arch. Pharm. (IF 5.1) Pub Date : 2024-04-05 Maira Hasnain Pasha, Humaira Yasmeen Gondal, Shanza Munir, Sami A. Alhussain, Magdi E. A. Zaki
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UHPLC‐MS/MS analysis, cytotoxic, enzyme inhibition, and antioxidant properties of Lantana camara L. extracts obtained by conventional and nonconventional methods Arch. Pharm. (IF 5.1) Pub Date : 2024-04-04 Aleksandra Cvetanović Kljakić, Biljana Lončar, Kouadio Ibrahime Sinan, Ouattara Katinan Etienne, Jelena Božunović, Uroš Gašić, Ismail Koyuncu, Ozgur Yuksekdag, Gokhan Zengin
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Exploration and biological evaluation of 20‐vinyl pregnenes: A step forward toward selective modulators of the estrogen receptor α signaling for breast cancer treatment Arch. Pharm. (IF 5.1) Pub Date : 2024-04-04 Victoria Malakhova, Alexander Scherbakov, Danila Sorokin, Hanna Leanavets, Yaraslau Dzichenka, Igor Zavarzin, Yulia Volkova
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Lemongrass essential oil micro‐ and nanoencapsulation for industrial application: Production techniques and potential applications Arch. Pharm. (IF 5.1) Pub Date : 2024-03-29 Thais Leticia Moreira da Silva, Flávio Luís Beltrame, Priscileila Colerato Ferrari
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New pyridine‐based chalcones and pyrazolines with anticancer, antibacterial, and antiplasmodial activities Arch. Pharm. (IF 5.1) Pub Date : 2024-03-29 Jonathan Ramírez‐Prada, Juan S. Rocha‐Ortiz, Marta I. Orozco, Pedro Moreno, Miguel Guevara, Mauricio Barreto, Maria E. Burbano, Sara Robledo, Maria del Pilar Crespo‐Ortiz, Jairo Quiroga, Rodrigo Abonia, Viviana Cuartas, Braulio Insuasty
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Synthesis, biological activities, and molecular docking studies of triazolo[4,3‐b]triazine derivatives as a novel class of α‐glucosidase and α‐amylase inhibitors Arch. Pharm. (IF 5.1) Pub Date : 2024-03-19 Soheila Seyfi, Somayeh Salarinejad, Setareh Moghimi, Mahsa Toolabi, Nastaran Sadeghian, Burak Tüzün, Loghman Firoozpour, Shima H. M. E. Ketabforoosh, Parham Taslimi, Alireza Foroumadi
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Screening of Chelidonium majus isoquinoline alkaloids reveals berberine and chelidonine as selective ligands for the nuclear receptors RORβ and HNF4α, respectively Arch. Pharm. (IF 5.1) Pub Date : 2024-03-19 Sohrab Salehi, Espen Schallmayer, Nils Bandomir, Annette Kärcher, Jan‐Frederik Güth, Pascal Heitel
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Health benefits of fraxetin: From chemistry to medicine Arch. Pharm. (IF 5.1) Pub Date : 2024-03-19 Nguyen Manh Ha, Ninh The Son
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Exploring rhodanine linked enamine–carbohydrazide derivatives as mycobacterial carbonic anhydrase inhibitors: Design, synthesis, biological evaluation, and molecular docking studies Arch. Pharm. (IF 5.1) Pub Date : 2024-03-18 Sarvan Maddipatla, Bulti Bakchi, Rutuja Rama Gadhave, Andrea Ammara, Shashikanta Sau, Bandela Rani, Srinivas Nanduri, Nitin Pal Kalia, Claudiu T. Supuran, Venkata Madhavi Yaddanapudi
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Sulfonamide‐incorporated bis(α‐aminophosphonates) as promising carbonic anhydrase inhibitors: Design, synthesis, biological evaluation, and X‐ray crystallographic studies Arch. Pharm. (IF 5.1) Pub Date : 2024-03-18 Marjan Sobati, Morteza Abdoli, Andrea Angeli, Alessandro Bonardi, Marta Ferraroni, Claudiu T. Supuran, Raivis Žalubovskis
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Morpholinodiazenyl chalcone blocks influenza A virus capsid uncoating by perturbing the clathrin‐mediated vesicular trafficking pathway Arch. Pharm. (IF 5.1) Pub Date : 2024-03-16 Ahammed A. Thottasseri, Gaganpreet Kaur, Deepthi Ramesh, Indranil Banerjee, Tharanikkarasu Kannan
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N1‐Benzoylated 5‐(4‐pyridinyl)indazole‐based kinase inhibitors: Attaining haspin and Clk4 selectivity via modulation of the benzoyl substituents Arch. Pharm. (IF 5.1) Pub Date : 2024-03-13 Habiba G. Aboelfotouh, Mennatallah Abdallah, Hend Khalifa, Youssef Aboushady, Ashraf H. Abadi, Matthias Engel, Mohammad Abdel‐Halim
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Design, synthesis, structure elucidation, antimicrobial, molecular docking, and SAR studies of novel urea derivatives bearing tricyclic aromatic hydrocarbon rings Arch. Pharm. (IF 5.1) Pub Date : 2024-03-11 Farid M. Sroor, Ahmed F. El‐Sayed, Mohamed Abdelraof
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Design, synthesis, and biological evaluation of 3‐benzenesulfonamide‐linked 3‐hydrazinoisatin derivatives as carbonic anhydrase inhibitors Arch. Pharm. (IF 5.1) Pub Date : 2024-03-11 Baijayantimala Swain, Vaibhav S. Marde, Priti Singh, Andrea Angeli, Abrar Khan, Venkata M. Yaddanapudi, Qasim Ullah, Claudiu T. Supuran, Mohammed Arifuddin
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Design and synthesis of highly selective Janus kinase 3 covalent inhibitors for the treatment of rheumatoid arthritis Arch. Pharm. (IF 5.1) Pub Date : 2024-03-05 Hualiang Yao, Jie Zhang, Qisheng Zheng, Xianxia Zeng, Huaizheng Huang, Zhen Ling, Minghai Tang, Zhiquan Chen, Wenchu Wang, Linhong He
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4‐{3‐[(Pyridin‐4‐ylmethyl)amino]‐[1,2,4]triazolo[4,3‐b][1,2,4]triazin‐6‐yl}phenol: An improved anticancer agent in hepatocellular carcinoma and a selective MDR1/MRP modulator Arch. Pharm. (IF 5.1) Pub Date : 2024-03-05 Zahra Zakeri Khatir, Antonella Di Sotto, Ester Percaccio, Tuba Tuylu Kucukkilinc, Ayse Ercan, Ann M. Chippindale, Mehdi Valipour, Hamid Irannejad
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A decade's overview of 2‐aminothiophenes and their fused analogs as promising anticancer agents Arch. Pharm. (IF 5.1) Pub Date : 2024-03-05 Donia G. Darwish, Hany A. M. El‐Sherief, Salah A. Abdel‐Aziz, Gamal El‐Din A. Abuo‐Rahma
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Novel benzene sulfonamides with acetylcholinesterase and carbonic anhydrase inhibitory actions Arch. Pharm. (IF 5.1) Pub Date : 2024-03-01 Rafika El Ati, Necla Öztaşkın, Ahmet Çağan, Akın Akıncıoğlu, Yeliz Demir, Süleyman Göksu, Rachid Touzani, İlhami Gülçin
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A comparative untargeted metabolomic analysis and assessment of antiplasmodial potential of nine Albizia species Arch. Pharm. (IF 5.1) Pub Date : 2024-02-27 Yosra A. El Khodary, Iriny M. Ayoub, Pierre Pério, Sandra Bourgeade‐Delmas, Nehal Ibrahim, Sherweit H. El‐Ahmady
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Targeting Lewy body dementia with neflamapimod‐rasagiline hybrids Arch. Pharm. (IF 5.1) Pub Date : 2024-02-27 Claudia Albertini, Sabrina Petralla, Francesca Massenzio, Barbara Monti, Nicola Rizzardi, Christian Bergamini, Elisa Uliassi, Fernanda Borges, Daniel Chavarria, Gert Fricker, Marcia Goettert, Thales Kronenberger, Matthias Gehringer, Stefan Laufer, Maria L. Bolognesi
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Chemical composition and biological activities of Cucurbita okeechobeensis extracts from its aerial parts, seeds, and fruit shells Arch. Pharm. (IF 5.1) Pub Date : 2024-02-26 Eulogio J. Llorent‐Martínez, Antonio Ruiz‐Medina, Milena Terzic, Kouadio Ibrahime Sinan, Ismail Koyuncu, Kadir Egi, Nilofar Nilofar, Gokhan Zengin
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Quinoa as phytopharmaceutical? Urinary elimination of ecdysterone after consumption of quinoa alone and in combination with spinach Arch. Pharm. (IF 5.1) Pub Date : 2024-02-24 Eduard Isenmann, Tasha Yuliandra, Konstantina Touvleliou, Matthias Broekmann, Xavier de la Torre, Francesco Botrè, Patrick Diel, Maria Kristina Parr
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Ligandability assessment of the C‐terminal Rel‐homology domain of NFAT1 Arch. Pharm. (IF 5.1) Pub Date : 2024-02-24 Jark Böttcher, Julian E. Fuchs, Moriz Mayer, Jan Kahmann, Krzysztof M. Zak, Tobias Wunberg, Simon Woehrle, Dirk Kessler
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Novel quinoline derivatives with broad‐spectrum antiprotozoal activities Arch. Pharm. (IF 5.1) Pub Date : 2024-02-24 Carla B. Hartman, Phelelisiwe S. Dube, Lesetja J. Legoabe, Natascha Van Pelt, An Matheeussen, Guy Caljon, Richard M. Beteck
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Rational design and synthesis of 2,4‐dichloro‐6‐methyl pyrimidine derivatives as potential selective EGFRT790M/L858R inhibitors for the treatment of non‐small cell lung cancer Arch. Pharm. (IF 5.1) Pub Date : 2024-02-21 Lei Duan, Cilong Chu, Xiaoling Huang, Huizhi Yao, Jie Wen, Rui Chen, Caolin Wang, Yuanbiao Tu, Qiaoli Lv, Qingshan Pan, Shan Xu
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Novel N-pyrocatechoyl and N-pyrogalloyl hydrazone antioxidants endowed with cytotoxic and antibacterial activity Arch. Pharm. (IF 5.1) Pub Date : 2024-02-12 Jovica Branković, Vesna Matejić, Dušica Simijonović, Milena D. Vukić, Miroslava Kačaniova, Marko Živanović, Ana Mirić, Jelena Košarić, Marija Branković, Vladimir P. Petrović
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Synthesis of novel benzylamine antimycotics and evaluation of their antimycotic potency Arch. Pharm. (IF 5.1) Pub Date : 2024-02-12 Monika Klimt, Martina Stadler, Ulrike Binder, Jürgen Krauss
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SiteMine: Large-scale binding site similarity searching in protein structure databases Arch. Pharm. (IF 5.1) Pub Date : 2024-02-09 Thorben Reim, Christiane Ehrt, Joel Graef, Sebastian Günther, Alke Meents, Matthias Rarey
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Advances in sample preparation methods for pesticide residue analysis in medicinal plants: A focus on Nepal Arch. Pharm. (IF 5.1) Pub Date : 2024-02-08 Sudip Pandey, Poonam Pant, Stefano Dall'Acqua
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A virtual library of small molecules mimicking dipeptides Arch. Pharm. (IF 5.1) Pub Date : 2024-02-08 Victor Jun Yu Lim, Hans-Dieter Gerber, Hannes Schihada, Van Tuan Trinh, Daniel Hilger, Olalla Vázquez, Peter Kolb
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Design, synthesis, and evaluation of dual-target inhibitors for the treatment of Alzheimer's disease Arch. Pharm. (IF 5.1) Pub Date : 2024-02-08 Jingfang Zhai, Canhua Hao, Xiaojing Wang, Yuexing Cao, Yinbo Pan, Min Zhou, Jie Sun, Chuanyou Li
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Sulfonyl thioureas with a benzo[d]thiazole ring as dual acetylcholinesterase/butyrylcholinesterase and human monoamine oxidase A and B inhibitors: An in vitro and in silico study Arch. Pharm. (IF 5.1) Pub Date : 2024-02-06 Nguyen Dinh Thanh, Do Son Hai, Vu Ngoc Toan, Hoang Thi Kim Van, Nguyen Thi Kim Giang, Nguyen Minh Tri
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Extracting binding energies and binding modes from biomolecular simulations of fragment binding to endothiapepsin Arch. Pharm. (IF 5.1) Pub Date : 2024-02-06 Birte Schmitz, Benedikt Frieg, Nadine Homeyer, Gisela Jessen, Holger Gohlke
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Dual COX-2 and 15-LOX inhibition study of novel 4-arylidine-2-mercapto-1-phenyl-1H-imidazolidin-5(4H)-ones: Design, synthesis, docking, and anti-inflammatory activity Arch. Pharm. (IF 5.1) Pub Date : 2024-02-05 Nermine A. Osman, Mostafa K. Soltan, Samar Rezq, Joseph Flaherty, Damian G. Romero, Ahmed S. Abdelkhalek
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UHPLC-ESI-QTOF-MS metabolite profiles of different extracts from Pelargonium endlicherianum parts and their biological properties based on network pharmacological approaches Arch. Pharm. (IF 5.1) Pub Date : 2024-02-05 Gokhan Zengin, Francisco Javier Leyva-Jiménez, Álvaro Fernández-Ochoa, Abdelhakim Bouyahya, Evren Yildiztugay, Antonio Segura Carretero, Mohamad Fawzi Mahomoodally, Sathish Kumar M Ponniya, Nilofar, Ismail Koyuncu, Özgür Yüksekdağ, María de la Luz Cádiz-Gurrea
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Multipathway regulation induced by 4-(phenylsulfonyl)morpholine derivatives against triple-negative breast cancer Arch. Pharm. (IF 5.1) Pub Date : 2024-02-05 Fan-Wei Yang, Te-Lun Mai, Ying-Chung Jimmy Lin, Yu-Chen Chen, Shang-Che Kuo, Chia-Ming Lin, Meng-Hsuan Lee, Jung-Chen Su
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Quinazoline-chalcone hybrids as HDAC/EGFR dual inhibitors: Design, synthesis, mechanistic, and in-silico studies of potential anticancer activity against multiple myeloma Arch. Pharm. (IF 5.1) Pub Date : 2024-01-31 Mostafa A. Mansour, Asmaa M. AboulMagd, Samar H. Abbas, Mohamed Abdel-Aziz, Hamdy M. Abdel-Rahman
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Development and evaluation of 2,4-disubstituted-5-aryl pyrimidine derivatives as antibacterial agents Arch. Pharm. (IF 5.1) Pub Date : 2024-02-02 Hend Khalifa, Sari Rasheed, Jörg Haupenthal, Jennifer Herrmann, Yasmine M. Mandour, Ashraf H. Abadi, Matthias Engel, Rolf Müller, Anna K. H. Hirsch, Mohammad Abdel-Halim, Mostafa M. Hamed
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Valorization of Citrus peels: GC/MS-based metabolites profiling, multivariate analysis, and antiaging potential Arch. Pharm. (IF 5.1) Pub Date : 2024-01-30 Wafaa M. El Kady, Iriny M. Ayoub, Ahmed K. El Mehrate, Mohamed Emad, Mohamed Tarek, Ahmed El Gdeily, El-Romisaa Mohamed, Rana Medhat, Omar Mahmoud, Amira M. Gad, Alaa M. Danderawy, Ola L. Breaka, Nada E. Mosad, Safaa M. Gemeaha, Noha Fathallah
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Design, synthesis, and activity evaluation of novel multitargeted l-tryptophan derivatives with powerful antioxidant activity against Alzheimer's disease Arch. Pharm. (IF 5.1) Pub Date : 2024-01-30 Xianghao Zeng, Shaobing Cheng, Huilan Li, Haiyang Yu, Yushun Cui, Yuanying Fang, Shilin Yang, Yulin Feng
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Design, synthesis, and biological evaluation of naphthoylamide derivatives as inhibitors of STAT3 phosphorylation Arch. Pharm. (IF 5.1) Pub Date : 2024-01-31 JiaHao Lu, XiuYang Yan, WuJi Lai, Li-He Jiang, Li-Qun Shen, Ai-Qun Wu, Chengguang Zhao
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On the hunt for metalloenzyme inhibitors: Investigating the presence of metal-coordinating compounds in screening libraries and chemical spaces Arch. Pharm. (IF 5.1) Pub Date : 2024-01-26 Bruna Schuck, Ruth Brenk