Go to
current issue
-
Novel thiobarbiturates as potent urease inhibitors with potential antibacterial activity: Design, synthesis, radiolabeling and biodistribution study Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-09-12 Hanan Gaber Abdulwahab; Marwa F. Harras; Nagwan Galal El Menofy; Amany M. Hegab; Basma M. Essa; Adli AbdAllah Selim; Tamer M. Sakr; Heba S.A. El-Zahabi
-
Studies on fragment-based design of allosteric inhibitors of human factor XIa Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-09-13 Rio S. Boothello; Nehru Viji Sankaranarayanan; Daniel K. Afosah; Rajesh Karuturi; Rami A. Al-Horani; Umesh R. Desai
-
Synthesis and Optimisation of P3 Substituted Vinyl Sulfone-Based Inhibitors as Anti-Trypanosomal Agents Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-09-20 William Doherty; Nikoletta Adler; Thomas J. Butler; Andrew J.S. Knox; Paul Evans
-
Genetic Code Expansion in Mammalian Cells: a Plasmid System Comparison Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-09-19 Wenyuan Zhou; Joshua S. Wesalo; Jihe Liu; Alexander Deiters
-
COVID-19 therapy: What weapons do we bring into battle? Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-09-10 Sinara Mônica Vitalino de Almeida; José Cleberson Santos Soares; Keriolaine Lima dos Santos; Josival Emanuel Ferreira Alves; Amélia Galdino Ribeiro; Íris Trindade Tenório Jacob; Cindy Juliane da Silva Ferreira; Jéssica Celerino dos Santos; Jamerson Ferreira de Oliveira; Luiz Bezerra de Carvalho Junior; Maria do Carmo Alves de Lima
-
Design, synthesis and biological evaluation of vortioxetine derivatives as new COX-1/2 inhibitors in human monocytes Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-09-11 Maria Talmon; Raju D. Chaudhari; Hemant Suryavanshi; Nilkanta Chowdhury; Martina Quaregna; Arianna Pin; Angshuman Bagchi; Goutam Biswas; Luigia G. Fresu
-
Design, synthesis, and multitargeted profiling of N-benzylpyrrolidine derivatives for the treatment of Alzheimer’s disease Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-26 Priyanka Kumari Choubey; Avanish Tripathi; Piyoosh Sharma; Sushant Kumar Shrivastava
-
Evaluation of 1,1-cyclopropylidene as a thioether isostere in the 4-thio-thienopyrimidine (TTP) series of antimalarials Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-09-11 Robert D. Barrows; Jared T. Hammill; Michael C. Tran; Mofolusho O. Falade; Amy L. Rice; Christopher W. Davis; Thomas J. Emge; Paul R. Rablen; R. Kiplin Guy; Spencer Knapp
-
Non-cytotoxic 1,2,3-triazole tethered fused heterocyclic ring derivatives display Tax protein inhibition and impair HTLV-1 infected cells Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-09-08 Daiane Fernanda dos Santos; Denise Regina Bairros de Pilger; Charlotte Vandermeulen; Ricardo Khouri; Susimaire Pedersoli Mantoani; Paulo Sérgio Gonçalves Nunes; Peterson de Andrade; Ivone Carvalho; Jorge Casseb; Jean-Claude Twizere; Luc Willems; Lucio Freitas-Junior; Simone Kashima
-
Discovery and structure activity relationships of 7-benzyl triazolopyridines as stable, selective, and reversible inhibitors of myeloperoxidase Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-09-01 Scott A. Shaw; Benjamin P. Vokits; Andrew K. Dilger; Andrew Viet; Charles G. Clark; Lynn M. Abell; Gregory A. Locke; Gerald Duke; Lisa M. Kopcho; Ashok Dongre; Ji Gao; Arathi Krishnakumar; Sutjano Jusuf; Javed Khan; Steven A. Spronk; Michael D. Basso; Lei Zhao; Glenn H. Cantor; Ellen K. Kick
-
Inhibition of Mycobacterium tuberculosis InhA: Design, synthesis and evaluation of new di-triclosan derivatives Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-09-08 Tom Armstrong; Malcolm Lamont; Alice Lanne; Luke J. Alderwick; Neil R. Thomas
-
N-phenyl ureidobenzenesulfonates, a novel class of promising human dihydroorotate dehydrogenase inhibitors Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-09-04 Chahrazed Bouzriba; Lauriane Larcher; Mathieu Gagné-Boulet; Sébastien Fortin
-
Identification of diphenylalkylisoxazol-5-amine scaffold as novel activator of cardiac myosin Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-09-05 Pulla Reddy Boggu; Eeda Venkateswararao; Manoj Manickam; Niti Sharma; Jong Seong Kang; Sang-Hun Jung
-
Analogs of nitrofuran antibiotics are potent GroEL/ES inhibitor pro-drugs Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-30 Mckayla Stevens; Chris Howe; Anne-Marie Ray; Alex Washburn; Siddhi Chitre; Jared Sivinski; Yangshin Park; Quyen Q. Hoang; Eli Chapman; Steven M. Johnson
-
Tetrahydroquinolinyl phosphinamidates and phosphonamidates enhancing tolerance towards drought stress in crops via interaction with ABA receptor proteins Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-30 Jens Frackenpohl; Luka J.B. Decker; Jan Dittgen; Jörg Freigang; Pierre Génix; Hendrik Helmke; Gudrun Lange; Peter Luemmen; Jana Schmidt; Dirk Schmutzler; Jean-Pierre Vors
-
Design and synthesis of Coenzyme A analogues as Aurora kinase A inhibitors: An exploration of the roles of the pyrophosphate and pantetheine moieties Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-09-05 Fiona Bellany; Yugo Tsuchiya; Trang M. Tran; A.W. Edith Chan; Helen Allan; Ivan Gout; Alethea B. Tabor
-
Preparation and evaluation of soluble epoxide hydrolase inhibitors with improved physical properties and potencies for treating diabetic neuropathic pain Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-31 Kin Sing Stephen Lee; Jen C. Ng; Jun Yang; Sung-Hee Hwang; Christophe Morisseau; Karen Wagner; Bruce D. Hammock
-
Discovery of Novel Steroidal-Chalcone Hybrids with Potent and Selective Activity against Triple-Negative Breast Cancer Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-09-12 Qiangqiang Hou; Xin Lin; Xiang Lu; Chengfeng Bai; Hanlin Wei; Guoshun Luo; Hua Xiang
-
Fluorinated 2-Arylcyclopropan-1-amines – A new class of sigma receptor ligands Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-09-01 Benjamin Schinor; Svenja Hruschka; Constantin G. Daniliuc; Dirk Schepmann; Bernhard Wünsch; Günter Haufe
-
Druggable targets from coronaviruses for designing new antiviral drugs Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-09-08 Leandro Rocha Silva; Paulo Fernando da Silva Santos-Júnior; Júlia de Andrade Brandão; Letícia Anderson; Ênio José Bassi; João Xavier de Araújo-Júnior; Sílvia Helena Cardoso; Edeildo Ferreira da Silva-Júnior
-
Fragment based drug design and diversity-oriented synthesis of carboxylic acid isosteres Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-28 Martina Ferri; Manuel Alunno; Francesco Antonio Greco; Andrea Mammoli; Giorgio Saluti; Andrea Carotti; Roccaldo Sardella; Antonio Macchiarulo; Emidio Camaioni; Paride Liscio
-
Structural basis for stabilization of human telomeric G-quadruplex [d-(TTAGGGT)]4 by anticancer drug epirubicin Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-09-10 Ritu Barthwal; Shailja Raje; Kumud Pandav
-
Novel 2-amino-1,4-naphthoquinone hybrids: Design, synthesis, cytotoxicity evaluation and in silico studies Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-28 Maryam Gholampour; Hassan Seradj; Somayeh Pirhadi; Mehdi Khoshneviszadeh
-
Design and synthesis of analogues of the sphingosine-1-phosphate receptor 1 agonist IMMH001 with improved phosphorylation rate in human blood Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-26 Qiong Xiao; Minwan Hu; Si Chen; Zeyu Shi; Jinping Hu; Ping Xie; Dali Yin
-
Design, synthesis of novel 4,5-dihydroisoxazole-containing benzamide derivatives as highly potent FtsZ inhibitors capable of killing a variety of MDR Staphylococcus aureus Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-27 Di Song; Fangchao Bi; Nan Zhang; Yinhui Qin; Xingbang Liu; Yuetai Teng; Shutao Ma
-
Optimization of linear and cyclic peptide inhibitors of KEAP1-NRF2 protein-protein interaction Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-30 Stefania Colarusso; Daniele De Simone; Tommaso Frattarelli; Matteo Andreini; Mauro Cerretani; Antonino Missineo; Daniele Moretti; Sara Tambone; Georg Kempf; Martin Augustin; Stefan Steinbacher; Ignacio Munoz-Sanjuan; Larry Park; Vincenzo Summa; Licia Tomei; Alberto Bresciani; Celia Dominguez; Leticia Toledo-Sherman; Elisabetta Bianchi
-
Chemical constituents from Macleaya cordata (Willd) R. Br. and their phenotypic functions against a Parkinson’s disease patient-derived cell line Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-28 Duy Thanh Nguyen; Jamila Iqbal; Jianying Han; Gregory K. Pierens; Stephen A. Wood; George D. Mellick; Yunjiang Feng
-
Focused structure-activity relationship profiling around the 2-phenylindole scaffold of a cannabinoid type-1 receptor agonist-positive allosteric modulator: site-III aromatic-ring congeners with enhanced activity and solubility Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-29 Peter C. Schaffer; Pushkar M. Kulkarni; David R. Janero; Ganesh A. Thakur
-
Design and synthesis of new disubstituted benzoxazolone derivatives that act as iNOS inhibitors with potent anti-inflammatory activity against LPS-induced acute lung injury (ALI) Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-30 Li Tang; Xiao-hui Gao; Bei Zhao; Jie-ran Luo; Xin-yang Shi; Rui Ge; Shu-rong Ban; Qing-shan Li
-
Next generation quorum sensing inhibitors: Accounts on structure activity relationship studies and biological activities Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-29 Mahesh S. Majik; Umesh B. Gawas; Vinod K. Mandrekar
-
Generation, optimization and characterization of novel anti-prion compounds Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-25 Andrea Altieri; Evgeny A. Spiridonov; Semen I. Sivtzev; Daisuke Ishibashi; Silvia Biggi; Noriyuki Nishida; Emiliano Biasini; Alexander V. Kurkin
-
Crystal structure of Leishmania mexicana cysteine protease B in complex with a highly potent azadipeptide nitrile inhibitor Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-09-06 Jean F.R. Ribeiro; Lorenzo Cianni; Chan Li; Thomas G. Warwick; Daniela de Vita; Fabiana Rosini; Fernanda dos Reis Rocho; Felipe G.P. Martins; Peter W. Kenny; Jeronimo Lameira; Andrei Leitão; Jonas Emsley; Carlos A. Montanari
-
Disulfide bridge cross-linking between protein and the RNA backbone as a tool to study RNase H1 Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-09-06 Malwina Hyjek-Składanowska; Anna R. Stasińska; Agnieszka Napiórkowska; Aneta Bartłomiejczak; Punit P. Seth; Marcin K. Chmielewski; Marcin Nowotny
-
Design and synthesis of novel methoxypyridine-derived gamma-secretase modulators Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-09-01 Kevin D. Rynearson; Ronald N. Buckle; R. Jason Herr; Nicholas J. Mayhew; Xinchao Chen; William D. Paquette; Samuel A. Sakwa; Jinhai Yang; Keith D. Barnes; Phuong Nguyen; William C. Mobley; raham Johnson; Juinn H. Lin; Rudolph E. Tanzi; Steven L. Wagner
The evolution of gamma-secretase modulators (GSMs) through the introduction of novel heterocycles with the goal of aligning activity for reducing the levels of Aβ42 and properties consistent with a drug-like molecule are described. The insertion of a methoxypyridine motif within the tetracyclic scaffold provided compounds with improved activity for arresting Aβ42 production as well as improved properties
-
Synthesis and biological evaluation of novel flexible nucleoside analogues that inhibit flavivirus replication in vitro Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-31 Joy E. Thames; Charles D. Waters; Coralie Valle; Marcella Bassetto; Wahiba Aouadi; Baptiste Martin; Barbara Selisko; Arissa Falat; Bruno Coutard; Andrea Brancale; Bruno Canard; Etienne Decroly; Katherine L. Seley-Radtke
-
Discovery of DS34942424: An orally potent analgesic without mu opioid receptor agonist activity Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-18 Tsuyoshi Arita; Masayoshi Asano; Kazufumi Kubota; Yuki Domon; Nobuo Machinaga; Kousei Shimada
-
Synthesis and biological activity of C-7, C-9 and C-10 modified taxane analogues from 1-deoxybaccatin VI Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-29 Chenghu Xie; Yongmei Cui; Lanlan Li; Minmin Zhang; Hongchun Liu; Haixia Lin
-
New BODIPYs for photodynamic therapy (PDT): synthesis and activity on human cancer cell lines Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-29 Enrico Caruso; Miryam C. Malacarne; Emanuela Marras; Ester Papa; Linda Bertato; Stefano Banfi; Marzia B. Gariboldi
-
Study on the interaction between 4-(1H-indol-3-yl)-2-(p-tolyl)quinazoline-3-oxide and human serum albumin Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-25 Yexiaoxu wang; Yi Liu; Qin Yang; Xuechun Mao; Wei-Ming Chai; Yiyuan Peng
-
Indole acrylonitriles as potential anti-hyperglycemic agents: Synthesis, α-glucosidase inhibitory activity and molecular docking studies Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-15 Mehwish Solangi; Kanwal; Khalid Mohammed Khan; Faiza Saleem; Shehryar Hameed; Jamshed Iqbal; Zainab Shafique; Urooj Qureshi; Zaheer Ul-Haq; Muhammad Taha; Shahnaz Perveen
-
Aminothiazolones as potent, selective and cell active inhibitors of the PIM kinase family Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-26 Camilo E. Quevedo; Carole J. R. Bataille; Simon Byrne; Matthew Durbin; Jon Elkins; Abigail Guillermo; Alan M. Jones; Stefan Knapp; Anna Nadali; Roderick G. Walker; Isabel Wilkinson; Graham M. Wynne; Stephen G. Davies; Angela J. Russell
-
Rational design of cell-permeable cyclic peptides containing a d-Pro-l-Pro motif Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-18 Jin Wen; Hui Liao; Kye Stachowski; Jordan P. Hempfling; Ziqing Qian; Chunhua Yuan; Mark P. Foster; Dehua Pei
-
Protection of all cleavable sites of DNA with the multiple CGCG or continuous CGG sites from the restriction enzyme, indicative of simultaneous binding of small ligands Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-25 Hirotaka Murase; Gentaro Wakisaka; Tomoharu Noguchi; Shigeki Sasaki
-
Fragment-based modification of 2,4-diarylaminopyrimidine derivatives as ALK and ROS1 dual inhibitors to overcome secondary mutants Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-25 Minglin Zhu; Wei Li; Tianming Zhao; Yuxiang Chen; Tong Li; Shangfei Wei; Ming Guo; Xin Zhai
-
A new naphthalene derivative with anti-amyloidogenic activity as potential therapeutic agent for Alzheimer's disease Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-11 Suchitil Rivera-Marrero; Alberto Bencomo-Martínez; Erika Orta Salazar; Marquiza Sablón-Carrazana; Laura García-Pupo; Florencia Zoppolo; Florencia Arredondo; Rosina Dapueto; María Daniela Santi; Ingrid Kreimerman; Tania Pardo; Laura Reyes; Lídice Galán; Samila León-Chaviano; Luis A. Espinosa-Rodríguez; Roberto Menéndez-Soto del Valle; Eduardo Savio; Sofía Díaz Cintra; Chryslaine Rodríguez-Tanty
-
Synthesis, Biological Evaluation and In Silico Modeling of Novel Pan-Genotypic NS5A Inhibitors Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-20 Andrey A. Ivashchenko; Yan A. Ivanenkov; Vladimir A. Aladinskiy; Ruben N. Karapetian; Angela G. Koryakova; Alexey A. Ryakhovskiy; Oleg D. Mitkin; Dmitry V. Kravchenko; Nikolai P. Savchuk; Bogdan A. Zagribelnyy; Alexander V. Ivashchenko
-
Pyrroformyl-containing 2,4-diaminopyrimidine derivatives as a new optimization strategy of ALK inhibitors combating mutations Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-20 Meng Cao; Yuxiang Chen; Tianming Zhao; Shangfei Wei; Ming Guo; Xin Zhai
-
Allosteric kidney-type glutaminase (GLS) inhibitors with a mercaptoethyl linker Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-06 Bridget Duvall; Sarah C. Zimmermann; Run-Duo Gao; Ajit G. Thomas; Filip Kalčic; Vijayabhaskar Veeravalli; Amira Elgogary; Rana Rais; Camilo Rojas; Anne Le; Barbara S. Slusher; Takashi Tsukamoto
-
The Splicing Modulator Sulfonamide Indisulam Reduces AR-V7 in Prostate Cancer Cells Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-18 James E. Melnyk; Veronica Steri; Hao G. Nguyen; Byron Hann; Felix Y. Feng; Kevan M. Shokat
-
Corrigendum to "Design, synthesis, and bioactivity of dihydropyrimidine derivatives as kinesin spindle protein inhibitors" [Bioorg. Med. Chem. 27 (2019) 115126]. Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-18 Haytham O Tawfik,Tarek F El-Moselhy,Nabaweya S El-Din,Mervat H El-Hamamsy
-
Exploring the physicochemical and antiproliferative properties of biaryl-linked [13]-macrodilactones Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-08 Chengsheng Chen; Cristin Bosko; Catherine P. McGeough; Ryan McLean; Angela M. Zaino; M. Kyle Hadden; Mark W. Peczuh
-
Widening the bottleneck: Heterologous expression, purification, and characterization of the Ktedonobacter racemifer minimal type II polyketide synthase in escherichia coli Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-15 Joshua G. Klein; Yang Wu; Bashkim Kokona; Louise K. Charkoudian
-
Small-molecule active pharmaceutical ingredients of approved cancer therapeutics inhibit human aspartate/asparagine-β-hydroxylase Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-06 Lennart Brewitz; Anthony Tumber; Xiaojin Zhang; Christopher J. Schofield
-
Dihydrobenzoxazinone derivatives as aldose reductase inhibitors with antioxidant activity Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-08 Huan Chen; Xin Zhang; Xiaonan Zhang; Zhenya Fan; Wenchao Liu; Yanqi Lei; Changjin Zhu; Bing Ma
-
Recent advances in the design of RAR α and RAR β agonists as orally bioavailable drugs. A review Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-07-29 Alan D. Borthwick; Maria B. Goncalves; Jonathan P.T. Corcoran
-
Design, synthesis and evaluation of a baicalin and berberine hybrid compound as therapeutic agent for ulcerative colitis Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-06 Dan Jia; Yonghui Dou; Ziwen Li; Xinxin Zhou; Ying Gao; Keji Chen; Weihong Cong; Min Ma; Zhengzhi Wu; Weimin Li
-
An orthogonal seryl-tRNA synthetase/tRNA pair for noncanonical amino acid mutagenesis in Escherichia coli Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-07-28 Claudio Zambaldo; Minseob Koh; Fariborz Nasertorabi; Gye Won Han; Abhishek Chatterjee; Raymond C. Stevens; Peter G. Schultz
-
Galangin ameliorated pulmonary fibrosis in vivo and in vitro by regulating epithelial-mesenchymal transition Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-07-28 Liqun Wang; Hongyao Liu; Qiurong He; Cailing Gan; Yali Li; Qianyu Zhang; Yuqin Yao; Fang He; Tinghong Ye; Wenya Yin
-
Improved design of peptides exhibiting angiogenic activities for clinical applications Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-02 Yuki Tominaga; Atsushi Kitagawa; Kiyoshi Nokihara
-
Design, synthesis and biological evaluation of 4-aryl-5-aminoalkyl-thiazole-2-amines derivatives as ROCK II inhibitors Bioorg. Med. Chem. (IF 3.073) Pub Date : 2020-08-03 Shuchao Ma; Linan Wang; Ben Ouyang; Meixia Fan; Junhui Qi; Lei Yao
Contents have been reproduced by permission of the publishers.
全部期刊列表>>
友情链接：
京公网安备 11010802027423号