title: Inhibition of neuronal nitric oxide synthase by 7-methoxyindazole and related substituted indazoles.
abstract: The synthesis and pharmacological evaluation of methoxyindazoles as new inhibitors of neuronal nitric oxide synthase are presented. The 7-methoxyindazole, although less potent than 7-NI, is the most active compound of the series in an in vitro enzymatic assay of neuronal nitric oxide synthase activity. This result shows that the nitro-substitution is not indispensable to the biological activity of the indazole ring. 7-Methoxyindazole possesses in vivo NOS inhibitory as well and related antinociceptive properties.
authors.affiliation: CNRS UMR 6551, Université de Caen, France. rault@pharmacie.unicaen.fr
authors.forename: P
authors.initials: P
authors.lastname: Schumann
authors.forename: V
authors.initials: V
authors.lastname: Collot
authors.forename: Y
authors.initials: Y
authors.lastname: Hommet
authors.forename: W
authors.initials: W
authors.lastname: Gsell
authors.forename: F
authors.initials: F
authors.lastname: Dauphin
authors.forename: J
authors.initials: J
authors.lastname: Sopkova
authors.forename: E T
authors.initials: ET
authors.lastname: MacKenzie
authors.forename: D
authors.initials: D
authors.lastname: Duval
authors.forename: M
authors.initials: M
authors.lastname: Boulouard
authors.forename: S
authors.initials: S
authors.lastname: Rault
mesh_terms: D000700:Analgesics / Q000138:chemical synthesis / Q000494:pharmacology; D000818:Animals; D001120:Arginine / Q000494:pharmacology; D002531:Cerebellum / Q000187:drug effects / Q000201:enzymology; D004305:Dose-Response Relationship, Drug; D004583:Electrons; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D007191:Indazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D051379:Mice; D019001:Nitric Oxide Synthase / Q000037:antagonists & inhibitors*; D052248:Nitric Oxide Synthase Type I; D010147:Pain Measurement / Q000187:drug effects; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: C436345:7-methoxyindazole; D000700:Analgesics; D004791:Enzyme Inhibitors; D007191:Indazoles; D001120:Arginine; D019001:Nitric Oxide Synthase; D052248:Nitric Oxide Synthase Type I; C496321:Nos1 protein, mouse; C496322:Nos1 protein, rat