Department of Pharmaceutical Chemistry, KLE University's College of Pharmacy, Nehru Nagar, Belgaum 590 010, Karnataka, India.
Bioorg Med Chem Lett. 2012 Mar 1;22(5):1917-21. doi: 10.1016/j.bmcl.2012.01.052. Epub 2012 Jan 26.
The increase in the prevalence of multi drug-resistant and extensively drug-resistant strains of Mycobacteriumtuberculosis case demonstrates the urgent need of discovering new promising compounds with antimycobacterial activity. As part of our research program and with a aim of identifying new antitubercular drug candidates, a new class of 2-(trifluoromethyl)-6-arylimidazo[2,1-b][1,3,4]thiadiazole derivatives has been synthesized by both conventional as well as microwave assisted method and evaluated for their in vitro antitubercular activity against M. tuberculosis H(37)Rv. Moreover, various drug-likeness properties of new compounds were predicted. Seven compounds from the series exhibited good activity with MIC in range 3.12-1.56μg/ml. The present study suggests that compounds 6b, 6c, 6d, 6e and 6f may serve as promising lead scaffolds for further generation of new anti-TB agents.
耐多药和广泛耐药结核分枝杆菌菌株的流行率增加表明，迫切需要发现具有抗分枝杆菌活性的新有前途的化合物。作为我们研究计划的一部分，旨在确定新的抗结核药物候选物，我们通过常规和微波辅助方法合成了一类新的 2-(三氟甲基)-6-芳基亚咪唑并[2,1-b][1,3,4]噻二唑衍生物，并评估了它们对结核分枝杆菌 H(37)Rv 的体外抗结核活性。此外，还预测了新化合物的各种药物相似性特性。该系列中有 7 种化合物表现出良好的活性，MIC 范围为 3.12-1.56μg/ml。本研究表明，化合物 6b、6c、6d、6e 和 6f 可作为进一步生成新型抗结核药物的有前途的先导骨架。
