Selective Inhibition of iNOS by Benzyl- and Dibenzyl Derivatives of N-(3-Aminobenzyl)acetamidine

被引：19

作者：

Fantacuzzi, Marialuigia ^{[1
]}

Maccallini, Cristina ^{[1
]}

Lannutti, Fabio ^{[1
]}

Patruno, Antonia ^{[1
]}

Masella, Simona ^{[1
]}

Pesce, Mirko ^{[2
]}

Speranza, Lorenza ^{[2
]}

Ammazzalorso, Alessandra ^{[1
]}

De Filippis, Barbara ^{[1
]}

Giampietro, Letizia ^{[1
]}

Re, Nazzareno ^{[1
]}

Amoroso, Rosa ^{[1
]}

机构：

[1] Univ G DAnnunzio, Dipartimento Sci Farmaco, I-66100 Chieti, Italy

[2] Univ G DAnnunzio, Dipartimento Sci Movimento Umano, I-66100 Chieti, Italy

来源：

CHEMMEDCHEM | 2011年 / 6卷 / 07期

关键词：

acetamidines; inhibitors; inducible nitric oxide synthases (NOS); isoform selectivity; nitric oxide; NITRIC-OXIDE SYNTHASE; BINDING; CLONING; EXPRESSION;

D O I：

10.1002/cmdc.201100125

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Picking your NOS: The effect of amine substitution at the 3-aminomethyl group of known iNOS inhibitor W1400 with mono- or disubstituted benzylic groups was evaluated. The o-nitro-benzyl derivative was identified as a potent inhibitor of iNOS, with good selectivity over eNOS. Docking simulations were performed to predict the binding mode of these derivatives in the iNOS and eNOS active sites. © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

引用

页码：1203 / 1206

页数：4

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