Synthesis and antibacterial activity of novel [1,2,4]triazolo [3,4-h][1,8]naphthyridine-7-carboxylic acid derivatives |
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Authors: | Liu-Zhou Gao Yu-Suo Xie Tao Li Wen-Long Huang Guo-Qiang Hu |
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Institution: | a Institute of Chemical Biology, Henan University, Kaifeng 475001, China;
b Centre of Drug Discovery, China Pharmaceutical University, Nanjing 210009, China |
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Abstract: | Novel tricyclic fluoroquinolones, 1,2,4]triazolo3,4-h]1,8]naphthyridine-8-one-7-carboxylic acid derivatives 4a-4h bearing carrying a functional Mannich-base moiety at the C-8 position, were synthesized and evaluated for their antimicrobial activity. The results showed that some compounds with a piperazine side chain exhibited comparable or better antibacterial activity than comparator cirprofloxacin. Furthermore, the targeted compounds also displayed a broad spectrum of activity against resistant strains including both Gram-negative and Gram-positive bacteria. In particular, compound 4h showed an MIC of 0.25 μg/mL in antibacterial assay against multiple drug-resistant Escherichia coli, which represents an about 30-fold increase of potency compared to ciprofloxacin. Thus, their excellent antibacterial activity against resistant strains suggests that triazole-fused fluoroquinolones warrant further optimization as novel anti-infective chemotherapies. |
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Keywords: | Triazole Tricyclic fluoroquinolone Synthesis Antibacterial activity |
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