Hepatitis C virus (HCV) NS5B polymerase is pivotal for replicating the viral RNA genome and is therefore an important target for therapeutic intervention of HCV infection.  Starting from our lead compound (2-(5-(2,4-dichlorobenzylidene)-4-oxo-2-thioxothiazolidin-3-yl)-3-phenylpropanoic acid, IC50 = 10.6 �M), we have carried out extensive SAR around the C-5-benzylidene substituent leading to the identification of (2-(5-(3-phenoxybenzylidene)-4-oxo-2-thioxothiazolidin-3-yl)-3-phenylpropanoic acid) with an IC50 value of 7.7 �M.  Further SAR optimization will be based on identification of optimal substituents at the phenoxy ring.  The synthesis, biological evaluation and SAR of these derivatives will be discussed.

Synthesis and SAR studies on rhodanine analogs as allosteric inhibitors of HCV NS5B polymerase

244th National Meeting (2012)

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