Literature DB >> 21592789

Indole 5-carboxamide Thumb Pocket I inhibitors of HCV NS5B polymerase with nanomolar potency in cell-based subgenomic replicons (part 2): central amino acid linker and right-hand-side SAR studies.

Pierre L Beaulieu1, Catherine Chabot, Jianmin Duan, Michel Garneau, James Gillard, Eric Jolicoeur, Martin Poirier, Marc-André Poupart, Timothy A Stammers, George Kukolj, Youla S Tsantrizos.   

Abstract

In this part 2, new indole 5-carboxamide Thumb Pocket 1 inhibitors of HCV NS5B polymerase are described. Structure-activity relationships (SAR) were explored at the central amino acid linker position and the right-hand-side of the molecule in an attempt to identify molecules with a balanced overall profile of potency (EC(50)<100 nM), physicochemical properties and ADME characteristics.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 21592789     DOI: 10.1016/j.bmcl.2011.04.082

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


  1 in total

1.  QSAR study of HCV NS5B polymerase inhibitors using the genetic algorithm-multiple linear regression (GA-MLR).

Authors:  Hamid Rafiei; Marziyeh Khanzadeh; Shahla Mozaffari; Mohammad Hassan Bostanifar; Zhila Mohajeri Avval; Reza Aalizadeh; Eslam Pourbasheer
Journal:  EXCLI J       Date:  2016-01-18       Impact factor: 4.068

  1 in total

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