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Synthesis and biological evaluation of novel fused indolo [3, 2-c] [1,8] naphthyridine derivatives as potential antibacterial agents
被引:8
|作者:
Makhanya, Talent Raymond
[1
]
Gengan, Robert Moonsamy
[1
]
Ata, Athar
[2
]
机构:
[1] Durban Univ Technol, Fac Sci Appl, Dept Chem, POB 1334,Steve Biko Campus, ZA-4001 Durban, South Africa
[2] Univ Winnipeg, Richardson Coll Environm Sci Complex, Dept Chem, Winnipeg, MB, Canada
基金:
新加坡国家研究基金会;
关键词:
Antibacterial activity;
indolo-naphthyridine;
mutagenicity;
Povarov reaction;
POVAROV REACTION-SYNTHESIS;
QUINOLINES;
INHIBITORS;
D O I:
10.1080/00397911.2019.1573373
中图分类号:
O62 [有机化学];
学科分类号:
070303 ;
081704 ;
摘要:
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 mu M 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. [GRAPHICS] .
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页码:823 / 835
页数:13
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