合成及生物评价黑尿酸酯作为新型人中性粒细胞弹性蛋白酶抑制剂。
Synthesis and biological evaluation of nigranoic acid esters as novel human neutrophil elastase inhibitors.
机构信息
a School of Chemistry and Chemical Engineering, Yunnan Normal University , Kunming 650050 , P.R. China.
出版信息
Nat Prod Res. 2015;29(17):1650-6. doi: 10.1080/14786419.2014.996149. Epub 2015 Jan 6.
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.
人中性粒细胞弹性蛋白酶 (HNE) 被认为是肺部疾病和其他炎症性疾病发病机制中的主要贡献者。我们有一系列的 12 种新的黑尼酸酯，通过区域选择性合成得到了良好的产率，并对其对 HNE 的抑制活性进行了评估。黑尼酸对 HNE 表现出显著的抑制活性，IC50 值为 3.77 μM，其中六种酯类对 HNE 具有相当的抑制作用，IC50 值在 2.61-8.95 μM 范围内。具有溴和三甲氧基取代苯基的黑尼酸酯 (3h 和 3b) 对 HNE 的抑制活性强于黑尼酸。
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