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Title: Synthesis and biological evaluation of indazole derivatives. Author: Claramunt RM, López C, López A, Pérez-Medina C, Pérez-Torralba M, Alkorta I, Elguero J, Escames G, Acuña-Castroviejo D. Journal: Eur J Med Chem; 2011 Apr; 46(4):1439-47. PubMed ID: 21334118. 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, E(rel), between stacking and apical interaction energies of indazoles with the active site of the NOS enzyme has been established.[Abstract] [Full Text] [Related] [New Search]