Synthesis and biological evaluation of indazole derivatives
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- 作者：Rosa M. Claramunt ; Concepció ; n Ló ; pez ; Ana Ló ; pez ; Carlos Pé ; rez-Medina ; Marta Pé ; rez-Torralba ; Ibon Alkorta ; José ; Elguero ; Germaine Escames ; Darí ; o Acuñ ; a-Castroviejo
- 关键词：Indazoles ; iNOS ; nNOS ; Modeling
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2011
- 出版时间：April 2011
- 年：2011
- 卷：46
- 期：4
- 页码：1439-1447
- 全文大小：566 K
文摘
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.