Literature DB >> 15357995

SAR and pharmacokinetic studies on phenethylamide inhibitors of the hepatitis C virus NS3/NS4A serine protease.

Savina Malancona1, Stefania Colarusso, Jesus M Ontoria, Antonella Marchetti, Marco Poma, Ian Stansfield, Ralph Laufer, Annalise Di Marco, Marina Taliani, Maria Verdirame, Odalys Gonzalez-Paz, Victor G Matassa, Frank Narjes.   

Abstract

SAR on the phenethylamide 1 (Ki 1.2 microM) in the P2- and the P'-position led to potent inhibitors, one of which showed good exposure and low clearance when administered intramuscularly to rat.

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Year:  2004        PMID： 15357995     DOI： 10.1016/j.bmcl.2004.05.093

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


  2 in total

1.  Drug resistance against HCV NS3/4A inhibitors is defined by the balance of substrate recognition versus inhibitor binding.

Authors:  Keith P Romano; Akbar Ali; William E Royer; Celia A Schiffer
Journal:  Proc Natl Acad Sci U S A       Date:  2010-11-17       Impact factor: 11.205

2.  High-throughput screening (HTS) and hit validation to identify small molecule inhibitors with activity against NS3/4A proteases from multiple hepatitis C virus genotypes.

Authors:  Hyun Lee; Tian Zhu; Kavankumar Patel; Yan-Yan Zhang; Lena Truong; Kirk E Hevener; Joseph L Gatuz; Gitanjali Subramanya; Hyun-Young Jeong; Susan L Uprichard; Michael E Johnson
Journal:  PLoS One       Date:  2013-10-09       Impact factor: 3.240
  2 in total

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