Monoamine Oxidase Inhibitory Activity of Novel Pyrazoline Analogues: Curcumin Based Design and Synthesis

被引：55

作者：

Badavath, Vishnu Nayak ^{[1
]}

Baysal, Ipek ^{[2
]}

Ucar, Gulberk ^{[2
]}

Sinha, Barij Nayan ^{[1
]}

Jayaprakash, Venkatesan ^{[1
]}

机构：

[1] Birla Inst Technol, Dept Pharmaceut Sci & Technol, Ranchi 835215, Jharkhand, India

[2] Hacettepe Univ, Fac Pharm, Dept Biochem, TR-06100 Ankara, Turkey

来源：

ACS MEDICINAL CHEMISTRY LETTERS | 2016年 / 7卷 / 01期

关键词：

Human monoamine oxidase; pyrazoline; enzyme inhibitors; molecular docking simulation; PARKINSONS-DISEASE; DERIVATIVES; ANTIDEPRESSANT; RATS; MAO; BROFAROMINE; MOCLOBEMIDE; DOPAMINE; FORMS; MICE;

D O I：

10.1021/acsmedchemlett.5b00326

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of new 2-methoxy-4-(5-pheny1-4,5dihydro-1H-pyrazol-3-yl)phenolderivatives, 4-13, were synthesized and tested for their human MAO inhibitory activity. All the compounds were found to be selective and reversible toward hMAO-A except 4, a selective inhibitor of hMAO-B and 12, a nonselective inhibitor. Compound 7 was found to be a potent inhibitor of hMAO-A with K-i = 0.06 +/- 0.003 mu M and was having selectivity index of (SI = 1.02 X 10(-5)). It was found to be better than standard drug, Moclobemide (hMAO-A with K = 0.11 +/- 0.01 mu M) with selectivity index of SI = 0.049. Molecular docking simulation was carried out to understand the crucial interactions responsible for selectivity and potency.

引用

页码：56 / 61

页数：6

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