title: 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.
abstract: We report a new class of non-nucleoside antivirals, the 7-oxo-4,7-dihydrothieno[3,2-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.
authors.affiliation: Pfizer Global Research and Development, 2800 Plymouth Rd., Ann Arbor, MI 48105, USA. scott.d.larsen@pfizer.com
authors.forename: Scott D
authors.initials: SD
authors.lastname: Larsen
authors.forename: Zhijun
authors.initials: Z
authors.lastname: Zhang
authors.forename: Brian A
authors.initials: BA
authors.lastname: DiPaolo
authors.forename: Peter R
authors.initials: PR
authors.lastname: Manninen
authors.forename: Douglas C
authors.initials: DC
authors.lastname: Rohrer
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Hageman
authors.forename: Todd A
authors.initials: TA
authors.lastname: Hopkins
authors.forename: Mary L
authors.initials: ML
authors.lastname: Knechtel
authors.forename: Nancee L
authors.initials: NL
authors.lastname: Oien
authors.forename: Bob D
authors.initials: BD
authors.lastname: Rush
authors.forename: Francis J
authors.initials: FJ
authors.lastname: Schwende
authors.forename: Kevin J
authors.initials: KJ
authors.lastname: Stefanski
authors.forename: Janet L
authors.initials: JL
authors.lastname: Wieber
authors.forename: Karen F
authors.initials: KF
authors.lastname: Wilkinson
authors.forename: Kathyrn M
authors.initials: KM
authors.lastname: Zamora
authors.forename: Michael W
authors.initials: MW
authors.lastname: Wathen
authors.forename: Roger J
authors.initials: RJ
authors.lastname: Brideau
mesh_terms: D003587:Cytomegalovirus / Q000201:enzymology*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D019384:Nucleic Acid Synthesis Inhibitors; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D019384:Nucleic Acid Synthesis Inhibitors; D011725:Pyridines; C023666:pyridine