School of Chemical Sciences, Swami Ramanand Teerth Marathwada University, Nanded 431606, India.
Bioorg Med Chem. 2013 Jan 1;21(1):365-72. doi: 10.1016/j.bmc.2012.09.060. Epub 2012 Nov 2.
Xanthine oxidase (XO) generates superoxide anions and H(2)O(2) for the self-defence system of organism. Abnormal production of this superoxide's (reactive oxygen species) is responsible for a number of complications including inflammation, metabolic disorder, cellular aging, reperfusion damage, atherosclerosis and carcinogenesis. Series of novel trisubstituted thiophenyl-1-thiazolyl-2-pyrazoline libraries are synthesized containing 2,5-dichloro thiophene, 5-chloro-2-(benzylthio) thiophene and 5-chlorothiophene-2-sulphonamide, from chalcones in PEG-400 as green solvent. Superoxide (XO) inhibitory and free radical scavenging activities were also figured out with molecular modeling analysis, bearing in mind their possible future for super oxide inhibitor (Gout) therapeutics, compound 3k shows interesting superoxide inhibitory and free radical scavenger activity with IC(50)=6.2 μM, in comparison with allopurinol.
黄嘌呤氧化酶(XO)为机体的自我防御系统产生超氧阴离子和 H(2)O(2)。这种超氧化物(活性氧)的异常产生与许多并发症有关,包括炎症、代谢紊乱、细胞衰老、再灌注损伤、动脉粥样硬化和致癌作用。从查耳酮在 PEG-400 中的绿色溶剂中合成了一系列新型三取代噻吩-1-噻唑基-2-吡唑啉库,其中包含 2,5-二氯噻吩、5-氯-2-(苄硫基)噻吩和 5-氯噻吩-2-磺酰胺。还通过分子建模分析研究了超氧化物(XO)抑制和自由基清除活性,考虑到它们在超氧化物抑制剂(痛风)治疗中的可能用途,化合物 3k 对超氧化物抑制和自由基清除具有有趣的活性,IC(50)=6.2μM,与别嘌醇相比。