Title:Synthesis and Evaluation of New 5-methylisoxazole-3-carboxamide Derivatives as Antitubercular Agents
VOLUME: 13 ISSUE: 2
Author(s):Neenu Ganesh, Gurubasavarj V. Pujar and Bharat K. Inturi
Affiliation:Department of Pharmaceutical Chemistry, JSS College of Pharmacy, JSS University, Mysore 570015, Karnataka, India.
Keywords:Antitubercular agents, antibacterial activity, bacillus subtilis, 5-methylisoxazole-3-carboxamide, MABA, mycobacterium
tuberculosis.
Abstract:Background: Tuberculosis is responsible for the world’s leading cause of death affecting
one third of the world’s population by the latent or dormant form despite the current chemotherapy.
For the effective management of MDR or XDR-TB, new lead compounds or novel therapeutic targets
are urgently needed. The present investigation is aimed at creating a new and hitherto unreported molecular
framework encompassing isoxazole moiety with carboxamide derivatives for the antitubercular
activity. Methods: 5-methylisoxazole-3-carboxamide derivatives (4-20) were synthesized in good yield
and were characterised by, spectral studies. In vitro antitubercular activity of the synthesized compounds
was determined against Mycobacterium tuberculosis H37Rv by MABA method and in vitro antibacterial activity
against Bacillus subtilis and Escherichia coli by serial dilution method. Results: The titled compounds, 10 and 14 showed
significant antitubercular activity with MIC of 3.125 µM and 9 and 13 with MIC of 6.25 μM among the tested compounds.
The active compounds have shown good safety profile against Vero and HepG2 Cell lines. The compounds 9, 13,
19 and 20 showed significant antibacterial activity with MIC of 6.25 µM and 15 and 17 showed activity with MIC of 12.5
µM among the tested compounds. Conclusion: In conclusion, we reported the convenient synthetic method for the
5-methylisoxazole-3-carboxamides. The results of antitubercular activity were encouraging. With structure base drug design
approach and suitable molecular modifications of the synthesized compounds 9, 10, 13 and 14, it is possible to develop
lead molecule with better antitubercular potential.
