Inhibitory effects of a series of 7-substituted-indazoles toward nitric oxide synthases: Particular potency of 1H-indazole-7-carbonitrile

…, B Ramassamy, L Alvey, M Lepoivre, Y Frapart…

Index: Cottyn, Betty; Acher, Francine; Ramassamy, Booma; Alvey, Luke; Lepoivre, Michel; Frapart, Yves; Stuehr, Dennis; Mansuy, Daniel; Boucher, Jean-Luc; Vichard, Dominique Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 11 p. 5962 - 5973

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Citation Number: 20

Abstract

A series of new 7-monosubstituted and 3, 7-disubstituted indazoles have been prepared and evaluated as inhibitors of nitric oxide synthases (NOS). 1H-Indazole-7-carbonitrile (6) was found equipotent to 7-nitro-1H-indazole (1) and demonstrated preference for constitutive NOS over inducible NOS. By contrast, 1H-indazole-7-carboxamide (8) was slightly less potent but demonstrated a surprising selectivity for the neuronal NOS. Further ...