期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 62, 期 -, 页码 508-514出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2012.11.046
关键词
3-(2-Bromoacetyl)coumarins; 2-(5-Hydroxy-5-trifluoromethyl-4,5-dihydropyrazol-1-yl)-4-(coumarin-3-yl) thiazoles; Anti-inflammatory activity; Antibacterial activity
资金
- Council of Scientific and Industrial Research, New Delhi
A series of novel 2-(5-hydroxy-5-trifluoromethyl-4,5-dihydropyrazol-1-yl)-4-(coumarin-3-yl)thiazoles (6) were synthesized by condensing 3-(2-bromoacetyl)coumarins (4) with various 5-hydroxy-5-trifluoromethyl-4,5-dihydropyrazol-1-thiocarboxamides (5), obtained by the reaction of thiosemicarbazide with trifluoromethyl-beta-diketones. All the tested compounds displayed significant to moderate in vivo anti-inflammatory activity when compared to the standard drug indomethacin, and good broad spectrum in vitro antibacterial activity against three Gram-positive and four Gram-negative bacteria when compared with cefixime. (C) 2013 Elsevier Masson SAS. All rights reserved.
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