Tri-substituted acylhydrazines as tertiary amide bioisosteres: HCV NS5B polymerase inhibitors |
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| Authors: | Canales Eda Carlson Joseph S Appleby Todd Fenaux Martijn Lee Johnny Tian Yang Tirunagari Neeraj Wong Melanie Watkins William J |
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| Institution: | Medicinal Chemistry Department, Gilead Sciences, 333 Lakeside Dr, Foster City, CA 94404, United States. eda.canales@gilead.com |
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| Abstract: | The use of a tri-substituted acylhydrazine as an isostere of a tertiary amide was explored in a series of HCV NS5B thumb site II inhibitors. Direct replacement generated an analog with similar conformational and physicochemical properties. The series was extended to produce compounds with potent binding affinities and encouraging levels of cellular potency. |
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