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Author Notes:

Raymond F. Schinazi Center for AIDS Research, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, and Veterans Affairs Medical Center, Decatur, GA 30033, USA rschina@emory.edu

Emory received no funding from RFS Pharma, LLC to perform this work and vice versa.

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Research Funding:

This work was supported in part by NIH grant 5P30-AI-50409 (CFAR), 5R01-AI-071846 and by the Department of Veterans Affairs. Dr. Schinazi is the founder and a major shareholder of RFS Pharma, LLC.

Keywords:

  • Science & Technology
  • Life Sciences & Biomedicine
  • Physical Sciences
  • Chemistry, Medicinal
  • Chemistry, Organic
  • Pharmacology & Pharmacy
  • Chemistry
  • NS5A
  • Antiviral
  • HCV
  • HEPATITIS-C
  • NUCLEOSIDE
  • CHEMISTRY
  • PROTEIN
  • DRUGS

Synthesis and evaluation of novel potent HCV NS5A inhibitors

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Journal Title:

Bioorganic and Medicinal Chemistry Letters

Volume:

Volume 22, Number 14

Publisher:

, Pages 4864-4868

Type of Work:

Article | Post-print: After Peer Review

Abstract:

Judicious modifications to the structure of the previously reported HCV NS5A inhibitor 1, resulted in more potent anti-HCV compounds with similar and in some cases improved toxicity profiles. The synthesis of 19 new NS5A inhibitors is reported along with their ability to block HCV replication in an HCV 1b replicon system. For the most potent compounds chemical stability, stability in liver microsomes and inhibition of relevant CYP450 enzymes is also presented.

Copyright information:

© 2012 Elsevier Ltd. All rights reserved.

This is an Open Access work distributed under the terms of the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License (http://creativecommons.org/licenses/by-nc-nd/4.0/).

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