Natural Product Research 2015-01-01

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

Guoli Huang, Li Feng, Bo Liu, Yi He, Yiming Li, Yegao Chen

文献索引：Nat. Prod. Res. 29 , 1650-6, (2015)

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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 3.77 μM, and six esters displayed considerable inhibitory effects on HNE with IC50 values in the range of 2.61-8.95 μM. The nigranoic acid esters having phenyls substituted with bromine and trimethoxyls (3h and 3b) showed stronger inhibitory activity on HNE than nigranoic acid.