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Updated: May 19, 2026

Synthesis of Antiviral Tetrahydrocarbazole Derivatives by Photochemical and Acid-catalyzed C-H Functionalization via Intermediate Peroxides (CHIPS)
Published on: June 20, 2014
Synthesis and SAR of pyridothiazole substituted pyrimidine derived HCV replication inhibitors
Vinay M Girijavallabhan1, Carmen Alvarez, Frank Bennett
1Merck Research Laboratories, 2015 Galloping Hill Rd., Kenilworth, NJ 07033, USA. vinay.girijavallabhan@spcorp.com
Abstract:
Introduction of a nitrogen atom into the benzene ring of a previously identified HCV replication (replicase) benzothiazole inhibitor 1, resulted in the discovery of the more potent pyridothiazole analogues 3. The potency and PK properties of the compounds were attenuated by the introductions of various functionalities at the R(1), R(2) or R(3) positions of the molecule (compound 3). Inhibitors 38 and 44 displayed excellent potency, selectivity (GAPDH/MTS CC(50)), PK parameters in all species studied, and cross genotype activity.
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