2. Academic Validation
  3. Active site inhibitors of HCV NS5B polymerase. The development and pharmacophore of 2-thienyl-5,6-dihydroxypyrimidine-4-carboxylic acid

Active site inhibitors of HCV NS5B polymerase. The development and pharmacophore of 2-thienyl-5,6-dihydroxypyrimidine-4-carboxylic acid

  • Bioorg Med Chem Lett. 2004 Oct 18;14(20):5085-8. doi: 10.1016/j.bmcl.2004.07.075.
Ian Stansfield 1,  Salvatore Avolio,  Stefania Colarusso,  Nadia Gennari,  Frank Narjes,  Barbara Pacini,  Simona Ponzi,  Steven Harper
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, IRBM/MRL Rome, Via Pontina Km 30,600, Pomezia, 00040 Rome, Italy.
PMID: 15380204 DOI: 10.1016/j.bmcl.2004.07.075
Abstract

5,6-Dihydroxypyrimidine-4-carboxylic acids are a promising series of hepatitis C virus (HCV) NS5B polymerase inhibitors that bind at the active site of the enzyme. Here we report a simple 2-thienyl substituted analogue that shows 10-fold improved activity over the original lead, and which allowed us to further delineate the key elements of the pharmacophore of this class of inhibitor. This work led to the identification of a trifluoromethyl acylsulfonamide group as a viable replacement for the C4 carboxylic acid in this series.

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