title: Novel thiazolo-pyrazolyl derivatives as xanthine oxidase inhibitors and free radical scavengers.
abstract: 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.
authors.affiliation: School of Life Sciences, Swami Ramanand Teerth Marathwada University, Nanded 431606 (MS), India.
authors.forename: Supriya D
authors.initials: SD
authors.lastname: Beedkar
authors.forename: Chandrahasya N
authors.initials: CN
authors.lastname: Khobragade
authors.forename: Santosh S
authors.initials: SS
authors.lastname: Chobe
authors.forename: Bhaskar S
authors.initials: BS
authors.lastname: Dawane
authors.forename: O S
authors.initials: OS
authors.lastname: Yemul
mesh_terms: D000493:Allopurinol / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D000818:Animals; D020134:Catalytic Domain; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D016166:Free Radical Scavengers / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D006073:Gout / Q000188:drug therapy; D020128:Inhibitory Concentration 50; D008958:Models, Molecular; D011720:Pyrazoles / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use; D051381:Rats; D013844:Thiazoles / Q000737:chemistry*; D014969:Xanthine Oxidase / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism
chemical_list: D004791:Enzyme Inhibitors; D016166:Free Radical Scavengers; D011720:Pyrazoles; D013844:Thiazoles; C031280:pyrazole; D000493:Allopurinol; D014969:Xanthine Oxidase