title: Substituted 2-aminopyridines as inhibitors of nitric oxide synthases.
abstract: A series of substituted 2-aminopyridines was prepared and evaluated as inhibitors of human nitric oxide synthases (NOS). 4,6-Disubstitution enhanced both potency and specificity for the inducible NOS with the most potent compound having an IC50 of 28 nM.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories Rahway, NJ 07065, USA. william_hagmann@merck.com
authors.forename: W K
authors.initials: WK
authors.lastname: Hagmann
authors.forename: C G
authors.initials: CG
authors.lastname: Caldwell
authors.forename: P
authors.initials: P
authors.lastname: Chen
authors.forename: P L
authors.initials: PL
authors.lastname: Durette
authors.forename: C K
authors.initials: CK
authors.lastname: Esser
authors.forename: T J
authors.initials: TJ
authors.lastname: Lanza
authors.forename: I E
authors.initials: IE
authors.lastname: Kopka
authors.forename: R
authors.initials: R
authors.lastname: Guthikonda
authors.forename: S K
authors.initials: SK
authors.lastname: Shah
authors.forename: M
authors.initials: M
authors.lastname: MacCoss
authors.forename: R M
authors.initials: RM
authors.lastname: Chabin
authors.forename: D
authors.initials: D
authors.lastname: Fletcher
authors.forename: S K
authors.initials: SK
authors.lastname: Grant
authors.forename: B G
authors.initials: BG
authors.lastname: Green
authors.forename: J L
authors.initials: JL
authors.lastname: Humes
authors.forename: T M
authors.initials: TM
authors.lastname: Kelly
authors.forename: S
authors.initials: S
authors.lastname: Luell
authors.forename: R
authors.initials: R
authors.lastname: Meurer
authors.forename: V
authors.initials: V
authors.lastname: Moore
authors.forename: S G
authors.initials: SG
authors.lastname: Pacholok
authors.forename: T
authors.initials: T
authors.lastname: Pavia
authors.forename: H R
authors.initials: HR
authors.lastname: Williams
authors.forename: K K
authors.initials: KK
authors.lastname: Wong
mesh_terms: D000631:Aminopyridines / Q000138:chemical synthesis* / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D019001:Nitric Oxide Synthase / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D000631:Aminopyridines; D004791:Enzyme Inhibitors; D019001:Nitric Oxide Synthase