The discovery and structure–activity relationships of pyrano[3,4-b]indole based inhibitors of hepatitis C virus NS5B polymerase

2010 ◽  
Vol 20 (9) ◽  
pp. 2968-2973 ◽  
Author(s):  
Matthew G. LaPorte ◽  
Tandy L. Draper ◽  
Lori E. Miller ◽  
Charles W. Blackledge ◽  
Lara K. Leister ◽  
...  
Keyword(s):  
Hepatitis C Virus ◽  
Hepatitis C ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Ns5b Polymerase

The discovery and structure–activity relationships of pyrano[3,4-b]indole-based inhibitors of hepatitis C virus NS5B polymerase

2011 ◽  
Vol 21 (11) ◽  
pp. 3227-3231 ◽  
Author(s):  
Randy W. Jackson ◽  
Matthew G. LaPorte ◽  
Torsten Herbertz ◽  
Tandy L. Draper ◽  
Janet A. Gaboury ◽  
...  
Keyword(s):  
Hepatitis C Virus ◽  
Hepatitis C ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Ns5b Polymerase

Novel Hepatitis C virus replicon inhibitors: Synthesis and structure–activity relationships of fused pyrimidine derivatives

2012 ◽  
Vol 22 (6) ◽  
pp. 2212-2215 ◽  
Author(s):  
A. Chris Krueger ◽  
Darold L. Madigan ◽  
David W. Beno ◽  
David A. Betebenner ◽  
Robert Carrick ◽  
...  
Keyword(s):  
Hepatitis C Virus ◽  
Hepatitis C ◽  
Pyrimidine Derivatives ◽  
Structure Activity Relationships ◽  
Structure Activity

Allosteric N-acetamide-indole-6-carboxylic acid thumb pocket 1 inhibitors of hepatitis C virus NS5B polymerase — Acylsulfonamides and acylsulfamides as carboxylic acid replacements

2013 ◽  
Vol 91 (1) ◽  
pp. 66-81 ◽  
Author(s):  
Pierre L. Beaulieu ◽  
René Coulombe ◽  
James Gillard ◽  
Christian Brochu ◽  
Jianmin Duan ◽  
...  
Keyword(s):  
Crystal Structure ◽  
Hepatitis C Virus ◽  
Hepatitis C ◽  
Carboxylic Acid ◽  
Allosteric Inhibitors ◽  
Subgenomic Replicon ◽  
Structure Activity ◽  
Hcv Ns5b ◽  
Acid Function ◽  
Ns5b Polymerase

Acylsulfonamide and acylsulfamide as surrogates for the carboxylic acid function of N-acetamide-indole-6-carboxylic acids were evaluated as allosteric inhibitors of hepatitis C virus (HCV) NS5B polymerase. Several analogs displayed excellent antiviral potency against both 1a and 1b HCV genotypes in cell-based subgenomic replicon assays. Structure–activity relationships (SAR) are discussed in the context of the crystal structure of an inhibitor − NS5B polymerase complex. Absorption, distribution, metabolism, and excretion pharmacokinetic (ADME-PK) properties of this class of inhibitors are also described.

Large-scale structure-activity relationship study of hepatitis C virus NS5B polymerase inhibition using SMILES-based descriptors

2015 ◽  
Vol 19 (4) ◽  
pp. 955-964 ◽  
Author(s):  
Apilak Worachartcheewan ◽  
Virapong Prachayasittikul ◽  
Alla P. Toropova ◽  
Andrey A. Toropov ◽  
Chanin Nantasenamat
Keyword(s):  
Hepatitis C Virus ◽  
Hepatitis C ◽  
Large Scale ◽  
Large Scale Structure ◽  
Structure Activity Relationship ◽  
Scale Structure ◽  
Activity Relationship ◽  
Structure Activity ◽  
Relationship Study ◽  
Ns5b Polymerase
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