Synthesis and Antitubercular activity of New Thiazolidinones with Pyrazinyl and Thiazolyl Scaffolds
作者:Sambhaji T. Dhumal、Amarsinh R. Deshmukh、Lalit D. Khillare、Manisha Arkile、Dhiman Sarkar、Ramrao A. Mane
DOI:10.1002/jhet.2552
日期:2017.1
extensively drug resistant tuberculosis has prompted to develop new molecular entities to treat the disease. A series of new 4‐thiazolidinones with pyrazinyl and thiazolyl scaffolds has been synthesized, and their antitubercular activity is reported. The title 4‐thiazolidinones, N‐(pyrazinyl substituted thiazoloylamino)‐2‐aryl‐4‐thiazolidinones (6a, 6b, 6c, 6d, 6e, 6f, 6g, 6h, 6i, 6j) have been first time
多药耐药性和广泛耐药性结核病的出现促使人们开发出治疗这种疾病的新分子实体。已经合成了一系列带有吡嗪基和噻唑基支架的新的4-噻唑烷酮,并报道了它们的抗结核活性。标题4-噻唑烷酮,N-(吡嗪基取代的噻唑烷氨基)-2-芳基-4-噻唑烷酮(6a,6b,6c,6d,6e,6f,6g,6h,6i,6j)是首次使用吡嗪酰胺作为起始原料通过五个连续步骤制备的。薄层色谱和光谱分析已证实了中间体(碳乙氧基噻唑,酰肼和偶氮甲碱)和标题噻唑烷酮(6a,6b,6c,6d,6e,6f,6g,6h,6i,6j)的纯度和结构,分别。已对细菌菌株结核分枝杆菌H37Ra和分枝杆菌BCG进行了新的4-噻唑烷酮的抗结核筛选使用不同浓度的化合物(6a,6b,6c,6d,6e,6f,6g,6h,6i,6j)的溶液,给出了筛选结果。化合物6a显示出显着的抗结核活性。