期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 65, 期 8, 页码 6171-6190出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.2c00001
关键词
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资金
- National Natural Science Foundation of China [21971212, 81450110095]
- Natural Science Foundation of Chongqing, China [cstc2019jcyj-msxmX0012]
Novel carbazole-oxadiazoles were developed as potential antibacterial agents and showed predominant inhibitory effects on both Gram-positive and -negative bacteria, especially in impeding the growth of MRSA and Pseudomonas aeruginosa ATCC 27853. The compounds exhibited low cytotoxicity and low tendency to develop resistance, and could disintegrate bacterial cell membranes to exert excellent antibacterial effects.
Novel carbazole-oxadiazoles were developed as new potential antibacterial agents to combat dreadful resistance. Some target compounds displayed predominant inhibitory effects on the tested Gram-positive and -negative bacteria, and carbazole-oxadiazoles 5g, 5i-k, 16a-c, and tetrazole analogues 23b-c were found to be efficient in impeding the growth of MRSA and Pseudomonas aeruginosa ATCC 27853 (MICs = 0.25-4 mu g/mL). Furthermore, compounds 5g and 23b-c not only possessed rapid bactericidal ability and low tendency to develop resistance but also exhibited low cytotoxic effects toward Hek 293T, HeLa, and red blood cells (RBCs), especially molecule 5g also showed low toxicity in vivo, which showed the therapeutic potential of these compounds. Further exploration indicated that compounds 5g, 5i, and 23b-c could disintegrate the integrity of bacterial cell membranes to leak the cytoplasmic contents, thus exerting excellent antibacterial effects. These facts mean that carbazole-based antibacterial agents might have bright prospects in confronting bacterial infections.
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