Facile synthesis of 1,3-thiazolidin-4-ones as antitubercular agents

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• 作者：Dnyaneshwar D. Subhedar^a ; Mubarak H. Shaikh^a ; Manisha A. Arkile^b ; Amar Yeware^b ; Dhiman Sarkar^b ; Bapurao B. Shingate^a ; ^{bapushingate@gmail.com" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Antitubercular ; Cytotoxicity ; Green protocol ; Multicomponent reaction
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：1 April 2016
• 年：2016
• 卷：26
• 期：7
• 页码：1704-1708
• 全文大小：1836 K

文摘

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.