by Claramunt, Rosa M, López, Concepción, López, Ana, Pérez-Medina, Carlos, Pérez-Torralba, Marta, Alkorta, Ibon, Elguero, José, Escames, Germaine and Acuña-Castroviejo, Darío
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.
Reference:
Synthesis and biological evaluation of indazole derivatives. (Claramunt, Rosa M, López, Concepción, López, Ana, Pérez-Medina, Carlos, Pérez-Torralba, Marta, Alkorta, Ibon, Elguero, José, Escames, Germaine and Acuña-Castroviejo, Darío), In European journal of medicinal chemistry, volume 46, 2011.
Bibtex Entry:
@article{claramunt_synthesis_2011,
	title = {Synthesis and biological evaluation of indazole derivatives.},
	volume = {46},
	url = {http://linkinghub.elsevier.com/retrieve/pii/S0223523411000493},
	doi = {10.1016/j.ejmech.2011.01.027},
	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.},
	language = {English},
	number = {4},
	journal = {European journal of medicinal chemistry},
	author = {Claramunt, Rosa M and López, Concepción and López, Ana and Pérez-Medina, Carlos and Pérez-Torralba, Marta and Alkorta, Ibon and Elguero, José and Escames, Germaine and Acuña-Castroviejo, Darío},
	month = apr,
	year = {2011},
	pmid = {21334118},
	pages = {1439--1447}
}