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7-Oxo-4,7-dihydrothieno[3,2-b]pyridine-6-carboxamides: synthesis and biological activity of a new class of highly potent inhibitors of human cytomegalovirus DNA polymerase
Authors:Larsen Scott D  Zhang Zhijun  DiPaolo Brian A  Manninen Peter R  Rohrer Douglas C  Hageman Michael J  Hopkins Todd A  Knechtel Mary L  Oien Nancee L  Rush Bob D  Schwende Francis J  Stefanski Kevin J  Wieber Janet L  Wilkinson Karen F  Zamora Kathyrn M  Wathen Michael W  Brideau Roger J
Institution:Pfizer Global Research and Development, 2800 Plymouth Rd., Ann Arbor, MI 48105, USA. scott.d.larsen@pfizer.com
Abstract:We report a new class of non-nucleoside antivirals, the 7-oxo-4,7-dihydrothieno3,2-b]pyridine-6-carboxamides, some of which possess remarkable potency versus a broad spectrum of herpesvirus DNA polymerases and excellent selectivity compared to human DNA polymerases. A critical factor in the level of activity is hypothesized to be conformational restriction of the key 2-aryl-2-hydroxyethylamine sidechain by an adjacent methyl group.
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