title: Carbocyclic influenza neuraminidase inhibitors possessing a C3-cyclic amine side chain: synthesis and inhibitory activity.
abstract: As part of our continuing work in the area of influenza neuraminidase inhibitors, a series of C3-aza inhibitors possessing a cyclic amine side chain was synthesized and evaluated for influenza neuraminidase inhibitory activity. Analogues possessing a six-, seven- and eight-membered ring, 4c-e, respectively, at the C3 position exhibited excellent influenza B neuraminidase inhibition.
authors.affiliation: Gilead Sciences Inc., Foster City, CA 94404, USA. willard_lew@gilead.com
authors.forename: W
authors.initials: W
authors.lastname: Lew
authors.forename: H
authors.initials: H
authors.lastname: Wu
authors.forename: X
authors.initials: X
authors.lastname: Chen
authors.forename: B J
authors.initials: BJ
authors.lastname: Graves
authors.forename: P A
authors.initials: PA
authors.lastname: Escarpe
authors.forename: H L
authors.initials: HL
authors.lastname: MacArthur
authors.forename: D B
authors.initials: DB
authors.lastname: Mendel
authors.forename: C U
authors.initials: CU
authors.lastname: Kim
mesh_terms: D000588:Amines / Q000737:chemistry; D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D018360:Crystallography, X-Ray; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D009980:Influenza A virus / Q000187:drug effects* / Q000201:enzymology; D009981:Influenza B virus / Q000187:drug effects* / Q000201:enzymology; D009439:Neuraminidase / Q000037:antagonists & inhibitors*
chemical_list: D000588:Amines; D000998:Antiviral Agents; D004791:Enzyme Inhibitors; D009439:Neuraminidase