942589-57-3Relevant articles and documents
3-CARBONYLAMINOTHIOPHENE-2-CARBOXYLIC ACIDS AS HEPATITIS C VIRUS INHIBITORS
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Page/Page column 45, (2009/03/07)
The present invention relates to novel 2-carboxy thiophene compounds of the formula (I): and salts thereof, to pharmaceutical compositions containing them and their use in medicine, as anti-viral agents. Specifically, the present invention relates to comp
Discovery of thiophene-2-carboxylic acids as potent inhibitors of HCV NS5B polymerase and HCV subgenomic RNA replication. Part 2: Tertiary amides
Chan, Laval,Pereira, Oswy,Reddy, T. Jagadeeswar,Das, Sanjoy K.,Poisson, Carl,Courchesne, Marc,Proulx, Melanie,Siddiqui, Arshad,Yannopoulos, Constantin G.,Nguyen-Ba, Nghe,Roy, Caroline,Nasturica, Daniel,Moinet, Christophe,Bethell, Richard,Hamel, Martine,L'Heureux, Lucille,David, Maud,Nicolas, Olivier,Courtemanche-Asselin, Philippe,Brunette, Stephanie,Bilimoria, Darius,Bedard, Jean
, p. 797 - 800 (2007/10/03)
Further SAR studies on the thiophene-2-carboxylic acids are reported. These studies led to the identification of a series of tertiary amides that show inhibition of both HCV NS5B polymerase in vitro and HCV subgenomic RNA replication in Huh-7 cells. Structural insights about the bioactive conformation of this class of molecules were deduced from a combination of modeling and transferred NOE (trNOE) studies.