期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 27, 期 8, 页码 1721-1726出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2017.02.076
关键词
Anti-inflammatory activity; COX-2 selective; Carrageenan-induced rat paw edema; Molecular docking; 4,5,6,7-Tetrahydro[b]benzothiophene
资金
- University Grants Commission India
A series of 2-phenyl-4,5,6,7-tetrahydro[b]benzothiophene derivatives were synthesized and evaluated for in vitro COX inhibitory potential. Within the series, compounds 4a, 4j, 4k, and 4q were identified as potential and selective COX-2 inhibitors with COX-2 IC50 in 0.31-1.40 mu M range; COX-2 selectivity index (SI) = 48.8-183.8 range and they showed percent PGE-2 inhibitory activity in the range of 25.4-46.9. Further, compounds 4a, 4j, 4k and 4q displayed potent anti-inflammatory activity with percentage rise in paw volume ranging from 21.1-30.5 at 180 min, while celecoxib demonstrated 19.6 percentage rise at the same dose at 180 min in carrageenan-induced rat paw edema assay. Cell viability via MTT assay showed no cytotoxicity up to 80 mu M concentrations. Molecular docking study of potent compounds in the series showed Gscore comparable to celecoxib with similar binding orientation for the COX-2 active site which also corroborates the observed in vitro COX-2 inhibition. (C) 2017 Elsevier Ltd. All rights reserved.
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