Himaja Malipeddi1,
Asif A Karigar2 
,
Venkata Ramana Malipeddi2,
Mukesh S Sikarwar3
For correspondence:- Asif Karigar Email: asifmpharm@yahoo.com Tel:+00919880219415
Received: 23 January 2012 Accepted: 12 July 2012 Published: 16 August 2012
Citation: Malipeddi H, Karigar AA, Malipeddi VR, Sikarwar MS. Synthesis and Antitubercular Activity of Some Novel Thiazolidinone Derivatives. Trop J Pharm Res 2012; 11(4):611-620 doi: 10.4314/tjpr.v11i4.12
© 2012 The authors.
This is an Open Access article that uses a funding model which does not charge readers or their institutions for access and distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0) and the Budapest Open Access Initiative (http://www.budapestopenaccessinitiative.org/read), which permit unrestricted use, distribution, and reproduction in any medium, provided the original work is properly credited..
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.
Archives
News Updates
Fulltext in PDF