作为抗结核药物的1,3 - 噻唑烷 - 4 - 酮的简便合成
Facile synthesis of 1,3-thiazolidin-4-ones as antitubercular agents.
作者信息
Subhedar Dnyaneshwar D, Shaikh Mubarak H, Arkile Manisha A, Yeware Amar, Sarkar Dhiman, Shingate Bapurao B
机构信息
Department of Chemistry, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad 431 004, India.
Combichem Bioresource Center, Organic Chemistry Division, CSIR-National Chemical Laboratory, Pune 411 008, India.
出版信息
Bioorg Med Chem Lett. 2016 Apr 1;26(7):1704-8. doi: 10.1016/j.bmcl.2016.02.056. Epub 2016 Feb 20.
We have developed, highly efficient, one-pot, solvent-free, [Et3NH][HSO4] catalyzed multicomponent reaction protocol for the synthesis of 1,3-thiazolidin-4-ones in excellent yields. For the first time, the 1,3-thiazolidin-4-ones were evaluated in vitro for their antimycobacterial activity against Mycobacterium tuberculosis dormant MTB H37Ra and Mycobacterium bovis BCG strains. Among the synthesized basic 1,3-thiazolidin-4-ones, particularly the compounds 4c, 4d, 4e, 4f, 4h, 4i and 4j displays promising antitubercular activity along with no significant cytotoxicity against the cell lines MCF-7, A549 and HCT-116.
我们开发了一种高效、一锅法、无溶剂、由[Et3NH][HSO4]催化的多组分反应方案，用于以优异产率合成1,3-噻唑烷-4-酮。首次对1,3-噻唑烷-4-酮进行了体外抗分枝杆菌活性评估，测试其对结核分枝杆菌休眠MTB H37Ra和牛分枝杆菌卡介苗菌株的活性。在合成的碱性1,3-噻唑烷-4-酮中，特别是化合物4c、4d、4e、4f、4h、4i和4j表现出有前景的抗结核活性，并且对MCF-7、A549和HCT-116细胞系没有明显的细胞毒性。
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