Trisubstituted thiophene analogues of 1-thiazolyl-2-pyrazoline, super oxidase inhibitors and free radical scavengers

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• 作者：Gajanan G. Mandawad^a ; Bhaskar S. Dawane^a ; ^{bhaskardawane@rediffmail.com} ; Supriya D. Beedkar^b ; Chandrahas N. Khobragade^b ; Omprakash S. Yemul^a
• 关键词：Thiophenyl thiazolyl pyrazoline ; Superoxide inhibitors ; Free radical scavengers ; Green synthesis ; PEG-400
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2013
• 出版时间：1 January, 2013
• 年：2013
• 卷：21
• 期：1
• 页码：365-372
• 全文大小：653 K

文摘

Xanthine oxidase (XO) generates superoxide anions and H₂O₂ 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 IC₅₀ = 6.2 ¦ÌM, in comparison with allopurinol.