4.4 Article

Synthesis and anti-inflammatory activity of some new 1,3,4-thiadiazoles containing pyrazole and pyrrole nucleus

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JOURNAL OF SAUDI CHEMICAL SOCIETY
卷 20, 期 -, 页码 S306-S312

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ELSEVIER SCIENCE BV
DOI: 10.1016/j.jscs.2012.11.007

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1,3,4-Acrylamides; 1,3,4-Thiadiazoles; Pyrrole-3-carboxamides; Pyrazole-3-carboxamides; Anti-inflammatory activity

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A new series of 1,3,4-thiadiazole with pyrazole-3-carboxamides (3a-f) and pyrrole-3-carboxamide (4a-f) moiety are prepared using intermediate compounds 1,3,4-thiadiazolacrylamides (2a-f). The structures of newly synthesized compounds were confirmed on the basis of their H-1 NMR, C-13 NMR, LCMS mass, FT-IR and elemental analysis data results. Among all the compounds (12), seven compounds were found to exhibit significant anti-inflammatory activity with 77.27, 75.89, 76.24, 68.55, 63.72, 57.41, 53.05% and 81.00, 80.55, 78.62, 71.45, 68.95, 61.89, 56.32% inhibition in paw edema at 3 h and 5 h respectively, compared to the standard drug indomethacin (74.82 and 80.32% at 3 h and 5 h). Compounds 3c, 3d and 4c exhibited potent activity than standard drug. (C) 2012 Production and hosting by Elsevier B.V. on behalf of King Saud University. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).

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