期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 45, 期 11, 页码 5120-5129出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2010.08.023
关键词
4-Isopropylthiazole; Triazolothiadiazoles; Triazolothiadiazines; Mannich bases; Cytotoxicity; Antitubercular
A series of novel clubbed Isopropylthiazole derivatives triazolothiadiazines 2a-g, dihydro triazolothiadiazoles 3a-g, thioxotriazoles 4a-d, triazolothiadiazole 5, arylideneamino triazolethiones 7a-h and oxadiazolethiones 11a-b were synthesized and characterized by IR, H-1 NMR, C-13 NMR, elemental and mass spectral analysis. These compounds were evaluated for their preliminary in vitro antibacterial, antifungal and antitubercular activity against Mycobacterium tuberculosis H(37)Rv strain by broth dilution assay method. All the compounds exhibited moderate to significant antibacterial and antifungal activities. Results of the antitubercular screening against M. tuberculosis H(37)Rv showed compounds 7c and 7d exhibited good antitubercular activity (MIC 4 and 8 mu g/mL) respectively, when compared with first line drug such as isoniazid (0.25 mu g/mL). (C) 2010 Elsevier Masson SAS. All rights reserved.
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