St Johns Pharmacy College, Department of Medicinal Chemistry, 6, 2nd stage Vijaynagar, R.P.C. Layout, Bangalore 560040, Karnataka, India.
Eur J Med Chem. 2010 Nov;45(11):5120-9. doi: 10.1016/j.ejmech.2010.08.023. Epub 2010 Aug 14.
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, (1)H NMR, (13)C 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 μg/mL) respectively, when compared with first line drug such as isoniazid (0.25 μg/mL).
一系列新型的异丁基噻唑衍生的三唑并噻二嗪 2a-g、二氢三唑并噻二嗪 3a-g、噻唑 4a-d、三唑并噻二嗪 5、芳基亚氨基三唑硫酮 7a-h 和恶二唑硫酮 11a-b 被合成并通过红外光谱 (IR)、（1）H 核磁共振谱 (1H NMR)、（13）C 核磁共振谱 (13C NMR)、元素分析和质谱分析进行了表征。这些化合物通过肉汤稀释法评估了它们对分枝杆菌 H(37)Rv 株的初步体外抗菌、抗真菌和抗结核活性。所有化合物均表现出中等至显著的抗菌和抗真菌活性。与异烟肼（0.25 μg/mL）等一线药物相比，抗结核筛选结果表明，化合物 7c 和 7d 具有良好的抗结核活性（MIC4 和 8 μg/mL）。
