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Tri-substituted acylhydrazines as tertiary amide bioisosteres: HCV NS5B polymerase inhibitors

✍ Scribed by Eda Canales; Joseph S. Carlson; Todd Appleby; Martijn Fenaux; Johnny Lee; Yang Tian; Neeraj Tirunagari; Melanie Wong; William J. Watkins


Book ID
116318565
Publisher
Elsevier Science
Year
2012
Tongue
English
Weight
459 KB
Volume
22
Category
Article
ISSN
0960-894X

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Conformational modeling has been successfully applied to the design of cyclic bioisosteres used to replace a conformationally rigid amide bond in a series of thiophene carboxylate inhibitors of HCV NS5B polymerase. Select compounds were equipotent with the original amide series. Single-point mutant