title: Trisubstituted thiophene analogues of 1-thiazolyl-2-pyrazoline, super oxidase inhibitors and free radical scavengers.
abstract: 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.
authors.affiliation: School of Chemical Sciences, Swami Ramanand Teerth Marathwada University, Nanded 431606, India.
authors.forename: Gajanan G
authors.initials: GG
authors.lastname: Mandawad
authors.forename: Bhaskar S
authors.initials: BS
authors.lastname: Dawane
authors.forename: Supriya D
authors.initials: SD
authors.lastname: Beedkar
authors.forename: Chandrahas N
authors.initials: CN
authors.lastname: Khobragade
authors.forename: Omprakash S
authors.initials: OS
authors.lastname: Yemul
mesh_terms: D000818:Animals; D001713:Biphenyl Compounds / Q000037:antagonists & inhibitors / Q000378:metabolism; D016166:Free Radical Scavengers / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D055772:Green Chemistry Technology; D062105:Molecular Docking Simulation; D010851:Picrates / Q000037:antagonists & inhibitors / Q000378:metabolism; D011092:Polyethylene Glycols / Q000737:chemistry; D051381:Rats; D017208:Rats, Wistar; D017382:Reactive Oxygen Species / Q000037:antagonists & inhibitors / Q000378:metabolism; D013481:Superoxides / Q000037:antagonists & inhibitors / Q000378:metabolism; D013876:Thiophenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D014969:Xanthine Oxidase / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D001713:Biphenyl Compounds; D016166:Free Radical Scavengers; D010851:Picrates; D017382:Reactive Oxygen Species; D013876:Thiophenes; D013481:Superoxides; D011092:Polyethylene Glycols; C004931:1,1-diphenyl-2-picrylhydrazyl; D014969:Xanthine Oxidase