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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, B. ; 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.

Bioorganic & medicinal chemistry letters, 2015-02, Vol.25 (4), p.944-947 [Periódico revisado por pares]

England: Elsevier Ltd

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Título:
Benzimidazole-containing HCV NS5A inhibitors: Effect of 4-substituted pyrrolidines in balancing genotype 1a and 1b potency
Autor: 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, B. ; 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.
Assuntos: Antiviral Agents - chemistry ; Antiviral Agents - pharmacology ; Benzimidazoles - chemistry ; Benzimidazoles - pharmacology ; Genotype ; HCV ; Hepatitis C virus ; NS5A ; Pyrrolidines - chemistry ; Pyrrolidines - pharmacology ; Viral Nonstructural Proteins - drug effects
É parte de: Bioorganic & medicinal chemistry letters, 2015-02, Vol.25 (4), p.944-947
Notas: ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
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Descrição: [Display omitted] 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.
Editor: England: Elsevier Ltd
Idioma: Inglês

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Benzimidazole-containing HCV NS5A inhibitors: Effect of 4-substituted pyrrolidines in balancing genotype 1a and 1b potency

England: Elsevier Ltd

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