Synthesis and biological evaluation of N-mercaptoacylcysteine derivatives as leukotriene A 4 hydrolase inhibitors

…, M Mizuchi, H Suhara, K Fujimura, M Horiuchi…

文献索引：Enomoto, Hiroshi; Morikawa, Yuko; Miyake, Yurika; Tsuji, Fumio; Mizuchi, Maki; Suhara, Hiroshi; Fujimura, Ken-ichi; Horiuchi, Masato; Ban, Masakazu Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 2 p. 442 - 446

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被引用次数: 12

摘要

We studied synthetic modifications of N-mercaptoacylamino acid derivatives to develop a new class of leukotriene A4 (LTA4) hydrolase inhibitors. S-(4-Dimethylamino) benzyl-l- cysteine derivative 2a (SA6541) showed inhibitory activity against LTA4 hydrolase (IC50, 270nM) and selectivity over other metallopeptidases except angiotensin-converting enzyme (ACE, IC50, 520nM). Modification at the para-substituent of the phenyl ring of compound ...