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Synthesis and biological evaluation of novel fused indolo [3, 2-c] [1,8] naphthyridine derivatives as potential antibacterial agents
Authors:Talent Raymond Makhanya  Robert Moonsamy Gengan  Athar Ata
Affiliation:1. Department of Chemistry, Faculty of Applied Science, Durban University of Technology, Durban, South Africa;2. Department of Chemistry, Richardson College for the Environmental Science Complex, The University of Winnipeg, Winnipeg, Manitoba, Canada
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.
Keywords:Antibacterial activity  indolo-naphthyridine  mutagenicity  Povarov reaction
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