title: Facile synthesis of 1,3-thiazolidin-4-ones as antitubercular agents.
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.
authors.affiliation: Department of Chemistry, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad 431 004, India.
authors.forename: Dnyaneshwar D
authors.initials: DD
authors.lastname: Subhedar
authors.affiliation: Department of Chemistry, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad 431 004, India.
authors.forename: Mubarak H
authors.initials: MH
authors.lastname: Shaikh
authors.affiliation: Combichem Bioresource Center, Organic Chemistry Division, CSIR-National Chemical Laboratory, Pune 411 008, India.
authors.forename: Manisha A
authors.initials: MA
authors.lastname: Arkile
authors.affiliation: Combichem Bioresource Center, Organic Chemistry Division, CSIR-National Chemical Laboratory, Pune 411 008, India.
authors.forename: Amar
authors.initials: A
authors.lastname: Yeware
authors.affiliation: Combichem Bioresource Center, Organic Chemistry Division, CSIR-National Chemical Laboratory, Pune 411 008, India.
authors.forename: Dhiman
authors.initials: D
authors.lastname: Sarkar
authors.affiliation: Department of Chemistry, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad 431 004, India. Electronic address: bapushingate@gmail.com.
authors.forename: Bapurao B
authors.initials: BB
authors.lastname: Shingate
mesh_terms: D000818:Animals; D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002460:Cell Line; D020650:Combinatorial Chemistry Techniques / Q000191:economics / Q000379:methods; D055772:Green Chemistry Technology / Q000191:economics / Q000379:methods; D006801:Humans; D008826:Microbial Sensitivity Tests; D009163:Mycobacterium bovis / Q000187:drug effects*; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D013329:Structure-Activity Relationship; D053778:Thiazolidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D014376:Tuberculosis / Q000188:drug therapy* / Q000662:veterinary
chemical_list: D000995:Antitubercular Agents; D053778:Thiazolidines
keywords: Antitubercular; Cytotoxicity; Green protocol; Multicomponent reaction