Novel thiazolo-pyrazolyl derivatives as xanthine oxidase inhibitors and free radical scavengers

被引:34
作者
Beedkar, Supriya D. [1 ]
Khobragade, Chandrahasya N. [1 ]
Chobe, Santosh S. [2 ]
Dawane, Bhaskar S. [2 ]
Yemul, O. S. [2 ]
机构
[1] Swami Ramanand Teerth Marathwada Univ, Sch Life Sci, Nanded 431606, MS, India
[2] Swami Ramanand Teerth Marathwada Univ, Sch Chem Sci, Nanded 431606, India
关键词
Thiazolo-pyrazolyl derivatives; alpha-Haloketones; Xanthine oxidase inhibition; Free radical scavengers; Molecular docking study; POLY(ETHYLENE GLYCOL) PEG; POLYETHYLENE-GLYCOL; GREEN PROCEDURE; SOLVENT; EFFICIENT; MECHANISM; PURINES; PEG-400; SYSTEM;
D O I
10.1016/j.ijbiomac.2012.02.009
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
070307 [化学生物学]; 071010 [生物化学与分子生物学];
摘要
Xanthine oxidase (XO) is a complex metalloflavoprotein, overproduction of which usually leads to a pathological condition called Gout. XO inhibitors may prove to be promising antigout agents. Present investigation describes synthesis, characterization and evaluation of 26 thiazolo-pyrazolyl derivatives V(a-z) for XO inhibitory and free radical scavenging activities. Derivatives Vq, Vo and Vh showed most promising XO inhibitory and free radical scavenging activities on the basis of their IC50 values ranging from (6.5-9 mu M). Significant dock scores compared with Allopurinol have been figured out using molecular docking. Evaluation of Vq, Vo and Vh for both the activities for first time may provide a new approach for antigout research. (C) 2012 Elsevier B.V. All rights reserved.
引用
收藏
页码:947 / 956
页数:10
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