Synthesis and biological evaluation of indazole derivatives

…, C Pérez-Medina, M Pérez-Torralba, I Alkorta…

Index: Claramunt, Rosa M.; Lopez, Concepcion; Lopez, Ana; Perez-Medina, Carlos; Perez-Torralba, Marta; Alkorta, Ibon; Elguero, Jose; Escames, Germaine; Acuna-Castroviejo, Dario European Journal of Medicinal Chemistry, 2011 , vol. 46, # 4 p. 1439 - 1447

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Citation Number: 15

Abstract

The inhibition of neuronal and inducible nitric oxide synthases (nNOS and iNOS) by a series of 36 indazoles has been evaluated, showing that most of the assayed derivatives are better iNOS than nNOS inhibitors. A parabolic model relating the iNOS inhibition percentage with the difference, Erel, between stacking and apical interaction energies of indazoles with the active site of the NOS enzyme has been established.