| Literature DB >> 25311566 |
Chetna Kharbanda1, Mohammad Sarwar Alam2, Hinna Hamid1, Kalim Javed1, Sameena Bano1, Abhijeet Dhulap3, Yakub Ali1, Syed Nazreen1, Saqlain Haider1.
Abstract
The present study aims at the synthesis of pyrazolines bearing benzothiazole and their evaluation as anti-inflammatory agents. The synthesized compounds were evaluated for their anti-inflammatory potential using carrageenan induced paw edema model. Two compounds 5a and 5d alleviated inflammation more than the standard drug celecoxib. Eight compounds 5 b, 5 c, 5 e, 5 g, 5 h, 6 b, 6 e and 6 f showed anti-inflammatory activity comparable to celecoxib. To understand the mode of action, COX-2 enzyme assay and TNF-α assay were carried out. All the active compounds were assessed for their cytotoxicity. The ulcerogenic risk evaluation was performed on the active compounds that were not found to be cytotoxic. Out of ten active compounds, two compounds (5 d and 6 f) were finally found to be the most potent anti-inflammatory agents attributing to the suppression of the COX-2 enzyme activity and TNF-α production without being either cytotoxic or ulcerogenic.Entities:
Keywords: Anti-inflammatory; COX-2; Molecular docking; Pyrazolines; TNF-α
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Year: 2014 PMID: 25311566 DOI: 10.1016/j.bmc.2014.09.028
Source DB: PubMed Journal: Bioorg Med Chem ISSN: 0968-0896 Impact factor: 3.641