Literature DB >> 19515564

Substituted benzothiadizine inhibitors of Hepatitis C virus polymerase.

Antony N Shaw1, Rosanna Tedesco, Ramesh Bambal, Deping Chai, Nestor O Concha, Michael G Darcy, Dashyant Dhanak, Kevin J Duffy, Duke M Fitch, Adam Gates, Victor K Johnston, Richard M Keenan, Juili Lin-Goerke, Nannan Liu, Robert T Sarisky, Kenneth J Wiggall, Michael N Zimmerman.   

Abstract

The synthesis and optimisation of HCV NS5B polymerase inhibitors with improved potency versus the existing compound 1 is described. Substitution in the benzothiadiazine portion of the molecule, furnishing improvement in potency in the high protein Replicon assay, is highlighted, culminating in the discovery of 12h, a highly potent oxyacetamide derivative.

Entities:  

Mesh:

Substances:

Year:  2009        PMID: 19515564     DOI: 10.1016/j.bmcl.2009.05.091

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  11 in total

1.  Preclinical characterization of GSK2336805, a novel inhibitor of hepatitis C virus replication that selects for resistance in NS5A.

Authors:  Jill Walker; Renae Crosby; Amy Wang; Ermias Woldu; Jessica Vamathevan; Christian Voitenleitner; Shihyun You; Katja Remlinger; Maoshang Duan; Wieslaw Kazmierski; Robert Hamatake
Journal:  Antimicrob Agents Chemother       Date:  2013-10-14       Impact factor: 5.191

2.  Preclinical characterization of JTK-853, a novel nonnucleoside inhibitor of the hepatitis C virus RNA-dependent RNA polymerase.

Authors:  Izuru Ando; Tsuyoshi Adachi; Naoki Ogura; Yukiyo Toyonaga; Kazuyuki Sugimoto; Hiroyuki Abe; Masafumi Kamada; Toru Noguchi
Journal:  Antimicrob Agents Chemother       Date:  2012-05-21       Impact factor: 5.191

Review 3.  Development of novel antiviral therapies for hepatitis C virus.

Authors:  Kai Lin
Journal:  Virol Sin       Date:  2010-07-28       Impact factor: 4.327

4.  Allosteric inhibitors have distinct effects, but also common modes of action, in the HCV polymerase.

Authors:  Brittny C Davis; Jodian A Brown; Ian F Thorpe
Journal:  Biophys J       Date:  2015-04-07       Impact factor: 4.033

5.  A cell-based assay for RNA synthesis by the HCV polymerase reveals new insights on mechanism of polymerase inhibitors and modulation by NS5A.

Authors:  C T Ranjith-Kumar; Yahong Wen; Nielson Baxter; Kanchan Bhardwaj; C Cheng Kao
Journal:  PLoS One       Date:  2011-07-22       Impact factor: 3.240

6.  Quantitative Structure-Activity Relationship Model for HCVNS5B inhibitors based on an Antlion Optimizer-Adaptive Neuro-Fuzzy Inference System.

Authors:  Mohamed Abd Elaziz; Yasmine S Moemen; Aboul Ella Hassanien; Shengwu Xiong
Journal:  Sci Rep       Date:  2018-01-24       Impact factor: 4.379

7.  Thumb inhibitor binding eliminates functionally important dynamics in the hepatitis C virus RNA polymerase.

Authors:  Brittny C Davis; Ian F Thorpe
Journal:  Proteins       Date:  2012-09-15

8.  In vitro characterization of GSK2485852, a novel hepatitis C virus polymerase inhibitor.

Authors:  Christian Voitenleitner; Renae Crosby; Jill Walker; Katja Remlinger; Jessica Vamathevan; Amy Wang; Shihyun You; John Johnson; Ermias Woldu; Stephanie Van Horn; Joseph Horton; Katrina Creech; J Brad Shotwell; Zhi Hong; Robert Hamatake
Journal:  Antimicrob Agents Chemother       Date:  2013-08-12       Impact factor: 5.191

9.  Discovery of Novel Hepatitis C Virus NS5B Polymerase Inhibitors by Combining Random Forest, Multiple e-Pharmacophore Modeling and Docking.

Authors:  Yu Wei; Jinlong Li; Jie Qing; Mingjie Huang; Ming Wu; Fenghua Gao; Dongmei Li; Zhangyong Hong; Lingbao Kong; Weiqiang Huang; Jianping Lin
Journal:  PLoS One       Date:  2016-02-04       Impact factor: 3.240

10.  New pyrazolobenzothiazine derivatives as hepatitis C virus NS5B polymerase palm site I inhibitors.

Authors:  Giuseppe Manfroni; Dinesh Manvar; Maria Letizia Barreca; Neerja Kaushik-Basu; Pieter Leyssen; Jan Paeshuyse; Rolando Cannalire; Nunzio Iraci; Amartya Basu; Maxim Chudaev; Claudio Zamperini; Elena Dreassi; Stefano Sabatini; Oriana Tabarrini; Johan Neyts; Violetta Cecchetti
Journal:  J Med Chem       Date:  2014-04-02       Impact factor: 7.446

View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.