Synthesis and biological evaluation of indazole derivatives

Rosa M. Claramunt, Concepción López, Ana López, Carlos Pérez-Medina, Marta Pérez-Torralba, Ibon Alkorta, José Elguero, Germaine Escames, Darío Acuña-Castroviejo

Research output: Contribution to journalArticlepeer-review

27 Scopus citations

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.

Original languageEnglish
Pages (from-to)1439-1447
Number of pages9
JournalEuropean Journal of Medicinal Chemistry
Volume46
Issue number4
DOIs
StatePublished - Apr 2011
Externally publishedYes

Keywords

  • Indazoles
  • Modeling
  • iNOS
  • nNOS

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