期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 49, 期 -, 页码 324-333出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2012.01.032
关键词
Benzothiazole; 1,2,3-Triazole; Click chemistry; bis-Heterocycles; Anti-inflammatory activity; COX
资金
- Hamdard National Foundation (HNF)
- Hamdard National fellowships
A focused library of novel bis-heterocycles encompassing 2-mercapto benzothiazole and 1,2,3-triazoles were synthesized using click chemistry approach. The synthesized compounds have been tested for their anti-inflammatory activity by using biochemical cyclooxygenase (COX) activity assays and carrageenan-induced hind paw edema. Among the tested compounds, compound 4d demonstrated a potent selective COX-2 inhibition with COX-2/COX-1 ratio of 0.44. Results from carrageenan-induced hind paw edema showed that compounds 4a, 4d, 4e and 4f posses significant anti-inflammatory activity as compared to the standard drug Ibuprofen. The compounds showing significant activity were further subjected to anti-nociceptive activity by writhing test. These four compounds have shown comparable activity with the standard Ibuprofen. Further ulcerogenic studies shows that none of these compounds causing gastric ulceration. (C) 2012 Elsevier Masson SAS. All rights reserved.
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