School of Life Sciences, Swami Ramanand Teerth Marathwada University, Nanded 431606 (MS), India.
Int J Biol Macromol. 2012 May 1;50(4):947-56. doi: 10.1016/j.ijbiomac.2012.02.009. Epub 2012 Feb 18.
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 IC(50) values ranging from (6.5-9 μM). 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.
黄嘌呤氧化酶(XO)是一种复杂的金属黄素蛋白,其过量产生通常会导致一种称为痛风的病理状况。XO 抑制剂可能被证明是有前途的抗痛风药物。本研究描述了 26 个噻唑并吡唑基衍生物 V(a-z) 的合成、表征和对 XO 抑制和自由基清除活性的评价。根据其 IC(50)值为(6.5-9 μM)的范围,衍生物 Vq、Vo 和 Vh 表现出最有前途的 XO 抑制和自由基清除活性。与别嘌醇相比,使用分子对接计算出了显著的对接分数。首次对 Vq、Vo 和 Vh 的这两种活性进行评估,可能为抗痛风研究提供一种新方法。