Literature DB >> 23177727

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

Gajanan G Mandawad1, Bhaskar S Dawane, Supriya D Beedkar, Chandrahas N Khobragade, Omprakash S Yemul.   

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.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID: 23177727     DOI: 10.1016/j.bmc.2012.09.060

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  3 in total

1.  Biological evaluation of synthetic chalcone and flavone derivatives as anti-inflammatory agents.

Authors:  Nelly Mateeva; Madhavi Gangapuram; Elizabeth Mazzio; Suresh Eyunni; Karam F A Soliman; Kinfe K Redda
Journal:  Med Chem Res       Date:  2015-04       Impact factor: 1.965

2.  Involvement of oxidative stress in SAMP10 mice with age-related neurodegeneration.

Authors:  Jun Wang; Hongtao Lei; Jincai Hou; Jianxun Liu
Journal:  Neurol Sci       Date:  2014-12-10       Impact factor: 3.307

3.  Synthesis and anti-nociceptive potential of isoxazole carboxamide derivatives.

Authors:  Hajira Bibi; Humaira Nadeem; Muzaffar Abbas; Muazzam Arif
Journal:  BMC Chem       Date:  2019-01-29
  3 in total

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