Synthesis and biological evaluation of novel fused indolo [3, 2-c] [1,8] naphthyridine derivatives as potential antibacterial agents

Abstract

Nine novel fused indolo [1,8] naphthyridine derivatives were synthesized using the Povarov reaction, in a one-pot system, and were fully characterized by spectroscopic techniques such as FT-IR, NMR, TOF-MS, and elemental analysis. Furthermore, their antibacterial activities against six bacterial strains were assessed. The results of the bioassay demonstrated that compounds 4a, 4c, and 4i showed good inhibitory effect with a MIC value ranging from 0.04687 to 0.09375 µM against Bacillus cereus and Staphylococcus aureus. The toxicity of 4a-i, evaluated through mutagenicity test against Salmonella typhimurium TA 98 and TA100 strains, revealed that there was no significant increase in the number of revertant colonies in comparison with the control, sodium azide.

Graphical Abstract

Keywords:

• Antibacterial activity
• indolo-naphthyridine
• mutagenicity
• Povarov reaction

Additional information

Funding

The authors thank the South African National Research Foundation, Durban University of Technology and the Canada Commonwealth Scholarship for financial assistance.