title: A new class of selective and potent inhibitors of neuronal nitric oxide synthase.
abstract: The synthesis and SAR of a series of 6-(4-(substituted)phenyl)-2-aminopyridines as inhibitors of nitric oxide synthase are described. Compound 3a from this series shows potent and selective inhibition of the human nNOS isoform, with pharmacokinetics sufficient to provide in vivo inhibition of nNOS activity.
authors.affiliation: Central Research Division, Pfizer Inc. Groton, CT 06340, USA.
authors.forename: J A
authors.initials: JA
authors.lastname: Lowe
authors.forename: W
authors.initials: W
authors.lastname: Qian
authors.forename: R A
authors.initials: RA
authors.lastname: Volkmann
authors.forename: S
authors.initials: S
authors.lastname: Heck
authors.forename: J
authors.initials: J
authors.lastname: Nowakowski
authors.forename: R
authors.initials: R
authors.lastname: Nelson
authors.forename: C
authors.initials: C
authors.lastname: Nolan
authors.forename: D
authors.initials: D
authors.lastname: Liston
authors.forename: K
authors.initials: K
authors.lastname: Ward
authors.forename: S
authors.initials: S
authors.lastname: Zorn
authors.forename: C
authors.initials: C
authors.lastname: Johnson
authors.forename: M
authors.initials: M
authors.lastname: Vanase
authors.forename: W S
authors.initials: WS
authors.lastname: Faraci
authors.forename: K A
authors.initials: KA
authors.lastname: Verdries
authors.forename: J
authors.initials: J
authors.lastname: Baxter
authors.forename: S
authors.initials: S
authors.lastname: Doran
authors.forename: M
authors.initials: M
authors.lastname: Sanders
authors.forename: M
authors.initials: M
authors.lastname: Ashton
authors.forename: P
authors.initials: P
authors.lastname: Whittle
authors.forename: M
authors.initials: M
authors.lastname: Stefaniak
mesh_terms: D000631:Aminopyridines / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D000818:Animals; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D006207:Half-Life; D019001:Nitric Oxide Synthase / Q000037:antagonists & inhibitors*; D052248:Nitric Oxide Synthase Type I; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D000631:Aminopyridines; D004791:Enzyme Inhibitors; D019001:Nitric Oxide Synthase; D052248:Nitric Oxide Synthase Type I; C496322:Nos1 protein, rat