Synthesis and antibacterial activity of some 5-hydroxy-5-trifluoromethyl-4,5-dihydropyrazol-1-thiocarboxamides, 3-trifluoromethylpyrazol-1-thiocarboxamides and 4-aryl-2-(5(3)-trifluoromethyl-1-pyrazolyl)thiazoles

被引：38

作者：

Aggarwal, Ranjana ^{[1
]}

Kumar, Rajiv ^{[1
]}

Kumar, Sunil ^{[1
]}

Garg, Gaurav ^{[2
]}

Mahajan, Ritu ^{[2
]}

Sharma, Jitender ^{[2
]}

机构：

[1] Kurukshetra Univ, Dept Chem, Kurukshetra 136119, Haryana, India

[2] Kurukshetra Univ, Dept Biotechnol, Kurukshetra 136119, Haryana, India

来源：

JOURNAL OF FLUORINE CHEMISTRY | 2011年 / 132卷 / 11期

关键词：

5-Hydroxy-5-trifluoromethyl-4,5-dihydropyrazol-1-thiocarboxamides; 3-Trifluoromethylpyrazol-1-thiocarboxamides; 3/5-Trifluoromethylpyrazolylthiazoles; Trifluoromethyl-beta-diketones; Thiosemicarbazide; Antibacterial activity; BIOLOGICAL EVALUATION; DEHYDRATION; INHIBITORS;

D O I：

10.1016/j.jfluchem.2011.07.029

中图分类号：

O61 [无机化学];

学科分类号：

070301 [无机化学];

摘要：

5-Hydroxy-5-trifluoromethyl-4,5-dihydropyrazol-1-thiocarboxamides 3 and 3-trifluoromethylpyrazol-1-thiocarboxamides 4, regioselectively obtained by the condensation of trifluoromethyl-beta-diketones with thiosemicarbazide under neutral and acidic conditions, on further reaction with phenacyl bromides 5 afforded 4-aryl-(5-trifluoromethyl-pyrazol-1-yl)thiazoles 6 and 4-aryl-(3-trifluoromethyl-pyrazol-1yl)thiazoles 7, respectively. Five 4,5-dihydropyrazoles (3a-e) and two pyrazolylthiazoles (6a and 6c) were tested against one Gram-positive and one Gram-negative bacteria to assess their in vitro antibacterial activity. Compounds 3a, 3b and 3e showed moderate antibacterial activity against Gram-positive bacterium, Bacillus pumilus. (C) 2011 Elsevier B.V. All rights reserved.

引用

页码：965 / 972

页数：8

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