Time-dependence and preliminary SAR studies in inhibition of nitric oxide synthase Isoforms by homologues of thiocitrulline

被引：6

作者：

Goodyer, CLM

Chinje, EC

Jaffar, M

Stratford, IJ

Threadgill, MD ^{[1
]}

机构：

[1] Univ Bath, Sch Pharm & Pharmacol, Bath BA2 7AY, Avon, England

[2] Univ Manchester, Sch Pharm & Pharmaceut Sci, Manchester M13 9PL, Lancs, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 21期

基金：

英国医学研究理事会;

关键词：

D O I：

10.1016/j.bmcl.2003.08.018

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Treatment of N-alpha-Cbz-N-epsilon-(2-hydroxyethylaminothiocarbonyl)-L-lysine N-(2-hydroxyethyl)amide with boiling hydrochloric acid gave N-epsilon-(4,5-dihydrothiazol-2-yl)-L-lysine. This was a weak and non-isoform selective inhibitor of NOS, whereas N-epsilon-aminothiocarbonyl-L-lysine and its methyl ester were potent, with IC50 = 13 and 18 muM, respectively, against human iNOS and IC50 = 3 and 8 muM, respectively, against rat nNOS. Time dependence was observed for inhibition of nNOS by the ester. (C) 2003 Elsevier Ltd. All rights reserved.

引用

收藏

页码：3679 / 3680

页数：2

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