化学
交易激励
吡格列酮
对接(动物)
吡唑
罗格列酮
噻唑烷二酮
过氧化物酶体增殖物激活受体
敌手
立体化学
药理学
受体
组合化学
生物化学
转录因子
2型糖尿病
基因
糖尿病
内分泌学
护理部
医学
作者
Mohd. Javed Naim,Ozair Alam,Md. Jahangir Alam,Md Quamrul Hassan,Nadeem Siddiqui,V.G.M. Naidu,Iqbal Alam
标识
DOI:10.1016/j.bioorg.2017.11.010
摘要
We herein report the design, synthesis and molecular docking studies of 2,4-thiazolidinedione derivatives containing benzene sulphonyl group which are docked against the Peroxisome Proliferator Activated Receptor (PPARγ) target. Compound 7p was most effective in lowering the blood glucose level as compared to standard drugs pioglitazone and rosiglitazone. Compound 7p exhibited potent PPAR-γ transactivation of 61.2% with 1.9 folds increase in gene expression. In molecular docking studies 7p showed excellent interactions with amino acids TYR 473, SER 289, HIE 449, TYR 327, ARG 288, MET 329 and LEU 228. Compound 7p did not cause any damage to the liver without any noteworthy weight gain and may be considered as promising candidates for the development of new antidiabetic agents.
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