Synthesis and pharmacological evaluation of some novel 2-(5-hydroxy-5-trifluoromethyl-4,5-dihydropyrazol-1-yl)-4-(coumarin-3-yl)thiazoles

被引：109
|
作者：
Aggarwal, Ranjana [1 ]
Kumar, Sunil [1 ]
Kaushik, Pawan [2 ]
Kaushik, Dhirender [2 ]
Gupta, Girish Kumar [3 ]
机构：
[1] Kurukshetra Univ, Dept Chem, Kurukshetra 136119, Haryana, India
[2] Kurukshetra Univ, Dept Pharmaceut Sci, Kurukshetra 136119, Haryana, India
[3] MM Univ, MM Coll Pharm, Mullana 133203, Ambala, India
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2013年 / 62卷
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; TRIFLUOROMETHYL-BETA-DIKETONES; ANTIBACTERIAL ACTIVITY; INHIBITORS; DESIGN; DERIVATIVES; THIAZOLES; AGENTS; DEHYDRATION; ANTICANCER; ANTITUMOR;
D O I：
10.1016/j.ejmech.2012.11.046
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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.
引用
收藏
页码：508 / 514
页数：7
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