1335316-22-7Relevant academic research and scientific papers
Benzimidazole-containing HCV NS5A inhibitors: Effect of 4-substituted pyrrolidines in balancing genotype 1a and 1b potency
Henderson, James A.,Bilimoria, Darius,Bubenik, Monica,Cadilhac, Caroline,Cottrell, Kevin M.,Dietrich, Evelyne,Denis, Francois,Ewing, Nigel,Falardeau, Guy,Giroux, Simon,Grey, Ronald,L'Heureux, Lucille,Liu, Bingcan,Mani, Nagraj,Morris, Mark,Nicolas, Olivier,Pereira, Oswy Z.,Poisson, Carl,Govinda Rao,Reddy, T. Jagadeeswar,Selliah, Subajini,Shawgo, Rebecca S.,Vaillancourt, Louis,Wang, Jian,Yannopoulos, Constantin G.,Chauret, Nathalie,Berlioz-Seux, Francoise,Chan, Laval C.,Das, Sanjoy K.,Grillot, Anne-Laure,Bennani, Youssef L.,Maxwell, John P.
, p. 944 - 947 (2015/02/19)
The treatment of HCV with highly efficacious, well-tolerated, interferon-free regimens is a compelling clinical goal. Trials employing combinations of direct-acting antivirals that include NS5A inhibitors have shown significant promise in meeting this challenge. Herein, we describe our efforts to identify inhibitors of NS5A and report on the discovery of benzimidazole-containing analogs with subnanomolar potency against genotype 1a and 1b replicons. Our SAR exploration of 4-substituted pyrrolidines revealed that the subtle inclusion of a 4-methyl group could profoundly increase genotype 1a potency in multiple scaffold classes.
ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS
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, (2011/10/13)
Compounds represented by formula I as described herein or pharmaceutically acceptable salts thereof, wherein A, B, B', X, Y, R1, R2, R2', R3, R3', R4, R4', R5, R5', m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.
