Synthesis and biological evaluation of indazole derivatives

被引：29

作者：

Claramunt, Rosa M. ^{[1
]}

Lopez, Concepcion ^{[1
]}

Lopez, Ana ^{[3
,4
]}

Perez-Medina, Carlos ^{[1
]}

Perez-Torralba, Marta ^{[1
]}

Alkorta, Ibon ^{[2
]}

Elguero, Jose ^{[2
]}

Escames, Germaine ^{[3
,4
]}

Acuna-Castroviejo, Dario ^{[3
,4
]}

机构：

[1] Univ Nacl Educ Distancia, Fac Ciencias, Dept Quim Organ & Bioorgan, E-28040 Madrid, Spain

[2] Ctr Quim Organ Manuel Lora Tamayo, CSIC, Inst Quim Med, E-28006 Madrid, Spain

[3] Univ Granada, Ctr Invest Biomed, E-18100 Granada, Spain

[4] Fac Med, Dept Fisiol, Granada 18012, Spain

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2011年 / 46卷 / 04期

关键词：

Indazoles; iNOS; nNOS; Modeling; NITRIC-OXIDE SYNTHASE; DENSITY FUNCTIONALS; RELAXING FACTOR; ENDOTHELIUM; INHIBITORS; SPECTROSCOPY; EXPRESSION; REACTIVITY; POTENCY; AZOLES;

D O I：

10.1016/j.ejmech.2011.01.027

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (c) 2011 Elsevier Masson SAS. All rights reserved.

引用

页码：1439 / 1447

页数：9

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