Literature DB >> 12419361

Design and synthesis of ethyl pyrrolidine-5,5-trans-lactams as inhibitors of hepatitis C virus NS3/4A protease.

Martin J Slater1, David M Andrews, Graham Baker, Susanne S Bethell, Seb Carey, Helene Chaignot, Berwyn Clarke, Barry Coomber, Malcolm Ellis, Andrew Good, Norman Gray, George Hardy, Paul Jones, Gail Mills, Ed Robinson.   

Abstract

Using a pyrrolidine-5,5-trans-lactam template, we have designed small, neutral, mechanism-based inhibitors of hepatitis C NS3/4A protease. Compound 11a, with an alpha-ethyl P1 substituent and a Boc-valine substituent at the pyrrolidine nitrogen, has an IC(50)=30 microM.

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Year:  2002        PMID: 12419361     DOI: 10.1016/s0960-894x(02)00789-8

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


  2 in total

1.  Development of cell-based assays for in vitro characterization of hepatitis C virus NS3/4A protease inhibitors.

Authors:  Victoria Chung; Anthony R Carroll; Norman M Gray; Nigel R Parry; Pia A Thommes; K Claire Viner; Eric A D'Souza
Journal:  Antimicrob Agents Chemother       Date:  2005-04       Impact factor: 5.191

2.  Investigation of some benzoquinazoline and quinazoline derivatives as novel inhibitors of HCV-NS3/4A protease: biological, molecular docking and QSAR studies.

Authors:  Hatem A Abuelizz; Mohamed Marzouk; Ahmed H Bakheit; Rashad Al-Salahi
Journal:  RSC Adv       Date:  2020-09-30       Impact factor: 4.036

  2 in total

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