European Journal of Biomedical and Pharmaceutical Sciences

NEW DIBROMOINDOLIZINE DERIVATIVES AS PROMISING ANTI-TB AGENTS WITH THEIR CYTOTOXICITY AND SAR STUDIES

Soumyashree D. K., Dinesh S. Reddy, Priyanka B. R., Pramod N. Patil and Basavaraj Padmashali

ABSTRACT

With the intent to discover new anti-TB agents, dibromoindolizine derivatives were synthesized (SA1-SA10). All the newly synthesized compounds were screened for their in vitro anti-tubercular activity, while the most active compounds were subjected to a cytotoxicity assay on Vero cell lines. From the overall data, it was found that compound (SA9) (MIC =1.50 μM) and (SA3) (MIC = 2.75 μM) were found to be more active than the standard drug pyrazinamide (MIC = 2.90 μM). It wasalso interesting to note that compounds (SA9) and (SA3) which showed remarkable anti-TBactivity were also found to exhibit the best safety profile against Vero cells indicating good selectivity profile. Hence further structuraloptimization of these hit candidates may lead to the discovery of more potent anti-TBagents. These data will help in developing and discovering morepotent and safer anti-TB agents with enhanced property.

Keywords: Indolizine, Anti-TB, cytotoxicity, SAR studies.