title: 4-substituted indazoles as new inhibitors of neuronal nitric oxide synthase.
abstract: A series of halo-1-H-indazoles has been synthesized and evaluated for its inhibitory activity on neuronal nitric oxide synthase. Introduction of bromine at the C4 position of the indazole ring system provided a compound almost as potent as the reference compound, that is, 7-nitroindazole (7-NI). The importance of position 4 is further demonstrated by the synthesis and pharmacological evaluation of the 4-nitroindazole which was also a potent inhibitor of NOS activity. These compounds also exhibited in vivo NOS inhibitory activity, as attested by potent antinociceptive effects following systemic administration.
authors: UPRES-EA 3915, Centre d'Etudes et de Recherche sur le Médicament de Normandie, UFR des Sciences Pharmaceutiques, rue Vaubénard, Caen, France.
authors: Michel
authors: M
authors: Boulouard
authors: Pascale
authors: P
authors: Schumann-Bard
authors: Sabrina
authors: S
authors: Butt-Gueulle
authors: Elodie
authors: E
authors: Lohou
authors: Silvia
authors: S
authors: Stiebing
authors: Valérie
authors: V
authors: Collot
authors: Sylvain
authors: S
authors: Rault
mesh_terms: D000818:Animals; D001966:Bromine / Q000737:chemistry; D002531:Cerebellum / Q000166:cytology / Q000187:drug effects / Q000201:enzymology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D007191:Indazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D009474:Neurons / Q000187:drug effects / Q000201:enzymology; D052248:Nitric Oxide Synthase Type I / Q000037:antagonists & inhibitors*; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D007191:Indazoles; D052248:Nitric Oxide Synthase Type I; D001966:Bromine; C080122:7-nitroindazole