2. Academic Validation
  3. Facile synthesis of 1,3-thiazolidin-4-ones as antitubercular agents

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

  • Bioorg Med Chem Lett. 2016 Apr 1;26(7):1704-8. doi: 10.1016/j.bmcl.2016.02.056.
Dnyaneshwar D Subhedar 1,  Mubarak H Shaikh 1,  Manisha A Arkile 2,  Amar Yeware 2,  Dhiman Sarkar 2,  Bapurao B Shingate 3
Affiliations

Affiliations

  • 1 Department of Chemistry, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad 431 004, India.
  • 2 Combichem Bioresource Center, Organic Chemistry Division, CSIR-National Chemical Laboratory, Pune 411 008, India.
  • 3 Department of Chemistry, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad 431 004, India. Electronic address: bapushingate@gmail.com.
PMID: 26927426 DOI: 10.1016/j.bmcl.2016.02.056
Abstract

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.

Keywords

Antitubercular; Cytotoxicity; Green protocol; Multicomponent reaction.

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