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Abstract

Synthesis and antimicrobial evaluation of some novel 2-imino-3-(4'-carboxamido pyridyl)-5-arylidene-4-thiazolidinones and their brominated derivatives

Author(s): P Mishra, T Lukose, SK Kashaw
Pharmaceutical Chemistry Division, Department of Pharmaceutical Sciences, Dr. H. S. Gour University, Sagar - 470 003, India

Correspondence Address:
S K Kashaw Pharmaceutical Chemistry Division, Department of Pharmaceutical Sciences, Dr. H. S. Gour University, Sagar - 470 003 India E-mail: [email protected]


Various novel 2-Imino-3-(4'-carboxamidopyridyl)-5-arylidene-4-thiazolidinones, structurally related to isonicotinic acid hydrazide (isoniazid) were synthesized and evaluated for their antimicrobial and antifungal activities together with their brominated products. Structure of the synthesized compounds was confirmed by means of their IR, 1 H-NMR spectral data and elemental analysis. Investigation of antimicrobial and antifungal activities of compounds was done by liquid dilution method used for the determination of minimum inhibitory concentration. Bacterial strains of Escherichia coli and Staphylococcus aureus and fungal strains of Aspergillus niger and Candida albicans were used to ascertain the activity whereas norfloxacin and amphotericin B was used as the standard positive control for antibacterial and antifungal activities respectively. MIC of the compounds ranged between 6-16 μg/ml and 7-24 μg/ml for antibacterial and antifungal activities respectively. Some of the synthesised compounds showed potent biological activities and were comparable to the standard. Important outcome of the exhaustive screening of all the new candidates in the present experiment was that the introduction of arylidene nuclei at position 5 of the 4-thiazolidinone nucleus significantly improved the biological activity.

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