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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