Article
Bicyclic octahydrocyclohepta[b]pyrrol-4(1H)one derivatives as novel selective anti-hepatitis C virus agents.
European journal of medicinal chemistry - 21 Oct 2016
Kaushik-Basu Neerja, Ratmanova Nina K, Manvar Dinesh, Belov Dmitry S, Cevik Ozge, Basu Amartya, Yerukhimovich Mark M, Lukyanenko Evgeny R, Andreev Ivan A, Belov Grigory M, Manfroni Giuseppe, Cecchetti Violetta, Frick David N, Kurkin Alexander V, Altieri Andrea, Barreca Maria Letizia
Abstract excerpt
We report the discovery of the bicyclic octahydrocyclohepta[b]pyrrol-4(1H)-one scaffold as a new chemotype with anti-HCV activity on genotype 1b and 2a subgenomic replicons. The most potent compound 34 displayed EC50 values of 1.8 μM and 4.5 μM in genotype 1b and 2a, respectively, coupled with the absence of any antimetabolic effect (gt 1b SI = 112.4; gt 2a SI = 44.2) in a cell-based assay. Compound 34 did not...
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