| Literature DB >> 27376494 |
Neerja Kaushik-Basu1, Nina K Ratmanova2, Dinesh Manvar3, Dmitry S Belov4, Ozge Cevik3, Amartya Basu3, Mark M Yerukhimovich5, Evgeny R Lukyanenko4, Ivan A Andreev4, Grigory M Belov4, Giuseppe Manfroni6, Violetta Cecchetti6, David N Frick5, Alexander V Kurkin7, Andrea Altieri8, Maria Letizia Barreca9.
Abstract
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 target HCV NS5B, IRES, NS3 helicase, or selected host factors, and thus future work will involve the unique mechanism of action of these new antiviral compounds.Entities:
Keywords: Anti-HCV agents; Aza-Cope–Mannich reaction; HCV inhibitors; Hepatitis C virus; Octahydrocyclohepta[b]pyrrol-4(1H)one derivatives
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Year: 2016 PMID： 27376494 DOI： 10.1016/j.ejmech.2016.06.041
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514