Synthesis and biological evaluation of nigranoic acid esters as novel human neutrophil elastase inhibitors

被引：6
|
作者：
Huang, Guoli [1 ]
Feng, Li [2 ]
Liu, Bo [1 ]
He, Yi [2 ]
Li, Yiming [2 ]
Chen, Yegao [1 ]
机构：
[1] Yunnan Normal Univ, Sch Chem & Chem Engn, Kunming 650050, Peoples R China
[2] Shanghai Univ Tradit Chinese Med, Sch Pharm, Shanghai 201203, Peoples R China
来源：
NATURAL PRODUCT RESEARCH | 2015年 / 29卷 / 17期
关键词：
nigranoic acid esters; human neutrophil elastase; inhibition; TRITERPENOIDS; HYDROXYLATION; MECHANISM;
D O I：
10.1080/14786419.2014.996149
中图分类号：
O69 [应用化学];
学科分类号：
081704 ;
摘要：
Human neutrophil elastase (HNE) has been implicated as a major contributor in the pathogenesis of diseases, such as lung disorders and other inflammatory diseases. A series of 12 new nigranoic acid esters were regioselectively synthesised in good yields and evaluated for HNE inhibitory activity. Nigranoic acid exhibited significant inhibitory activity against HNE with the IC50 value of 3.77M, and six esters displayed considerable inhibitory effects on HNE with IC50 values in the range of 2.61-8.95M. The nigranoic acid esters having phenyls substituted with bromine and trimethoxyls (3h and 3b) showed stronger inhibitory activity on HNE than nigranoic acid.
引用
收藏
页码：1650 / 1656
页数：7
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