HCV NS5AReplication Complex Inhibitors. Part 4.1 Optimization for Genotype 1a Replicon InhibitoryActivity.

A series of symmetrical E-stilbene prolinamidesthat originated from the library-synthesized lead 3wasstudied with respect to HCV genotype 1a (G-1a) and genotype 1b (G-1b)replicon inhibition and selectivity against BVDV and cytotoxicity.SAR emerging from an examination of the prolinamide cap region revealed 11to be a selective HCV NS5A inhibitor exhibiting submicromolarpotency against both G-1a and G-1b replicons. Additional structuralrefinements resulted in the identification of 30as apotent, dual G-1a/1b HCV NS5A inhibitor. [ABSTRACT FROM AUTHOR]