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The synthesis and evaluation of a novel class of (E)-3-(1-cyclohexyl-1H-pyrazol-3-yl)-2-methylacrylic acid hepatitis C virus polymerase NS5B inhibitors |
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| Authors: | Martin Scott W Glunz Peter Beno Brett R Bergstrom Carl Romine Jeffrey L Priestley E Scott Newman Makenzie Gao Min Roberts Susan Rigat Karen Fridell Robert Qiu Dike Knobloh Galina Wang Ying-Kai |
| Affiliation: | a Department of Chemistry, Bristol-Myers Squibb Research and Development, 5 Research Parkway Wallingford, CT 06492, United States b Computer-Assisted Drug Design Department, Applied Biotechnology, Bristol-Myers Squibb Research and Development, 5 Research Parkway Wallingford, CT 06492, United States c Department of Chemistry, Bristol-Myers Squibb Research and Development, 311 Penington-Rocky Hill Rd. Hopewell, NJ 08534, United States d Department of Virology, Bristol-Myers Squibb Research and Development, 5 Research Parkway Wallingford, CT 06492, United States |
| Abstract: | Herein we report the identification and evaluation of a novel series of (E)-3-(1-cyclohexyl-1H-pyrazol-3-yl)-2-methylacrylic acid derivatives identified from a deannulation study performed on the reported benzimidazole NS5B inhibitor, 1. This resulted in the identification of (E)-3-(2-(4-((4′-cyano-4-(4-hydroxypiperidine-1-carbonyl)biphenyl-2-yl)methoxy)phenyl)-1-cyclohexyl-1H-imidazol-4-yl)-2-methylacrylic acid (11) as a potent inhibitor of NS5B. Potential pathways for the further optimization of this series are suggested. |
| Keywords: | Hepatitis Polymerase NS5B Inhibitors Pyrazoles |
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