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

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• 作者：Supriya D. Beedkar^a ; Chandrahasya N. Khobragade^a ; ^{cnkhobragade@rediffmail.com} ; Santosh S. Chobe^b ; Bhaskar S. Dawane^b ; O.S. Yemul^b
• 关键词：Thiazolo-pyrazolyl derivatives ; 伪-Haloketones ; Xanthine oxidase inhibition ; Free radical scavengers ; Molecular docking study
• 刊名：International Journal of Biological Macromolecules
• 出版年：2012
• 期刊代码：62_01418130
• 类别：abs
• 出版时间：1 May, 2012
• 卷：50
• 期：4
• 页码：947-956
• 文件大小：970 K

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 渭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.