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Synthesis and Antitubercular Activity of Some Novel Thiazolidinone Derivatives
Malipeddi, Himaja; Karigar, Asif A; Malipeddi, Venkata Ramana & Sikarwar, Mukesh S
Abstract
Purpose: To synthesize and characterize novel thiazolidinone derivatives and screen them for
antitubercular activity.
Methods: A series of twelve novel thiazolidinones 4a-l have been synthesized by cyclocondensation of
various Schiff bases of amino thiadiazole with thioglycollic acid. Various Schiff bases 3a-l were
synthesized by condensation of 2-amino-5-aryl-5H-thiazolo[4,3-b]-l,3,4-thiadiazole with various aryl
aldehydes. The synthesized compounds were characterized by FTIR, 1H-NMR, 13C-NMR and mass
spectrometry. Docking studies were carried out for the synthesized compounds which were also
evaluated for in vitro anti-tubercular activity at a concentration of 0.1-100.0 μg/mL by Microplate Blue
Alamar Assay method. Pyrazinamide and streptomycin were used as standard antitubercular agents.
Results: The synthesized compounds showed good docking score, compared to standard drugs. Two
of the compounds (labelled 4f and 4i) showed higher antitubercular activity than the standards
(pyrazinamide and streptomycin) while compounds four others compounds (labeled 4b, 4c, 4e, 4h, 4k
and 4l) showed comparable activity to pyrazinamide but greater activity than streptomycin.
Conclusion: We report the successful synthesis of novel thiazolidinones, as well as their spectral
characterization, docking properties and in vitro antitubercular activities which, for some, are superior to
currently used anti-tubercular agents.
Keywords
Thiadiazole, Schiff base, Thiazolidinone, Anti-tubercular activity, Docking
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