Citation: Liu-Zhou Gao, Yu-Suo Xie, Tao Li, Wen-Long Huang, Guo-Qiang Hu. Synthesis and antibacterial activity of novel [1,2,4]triazolo [3,4-h][1,8]naphthyridine-7-carboxylic acid derivatives[J]. Chinese Chemical Letters, ;2015, 26(1): 149-151. doi: 10.1016/j.cclet.2014.09.017 shu

Synthesis and antibacterial activity of novel [1,2,4]triazolo [3,4-h][1,8]naphthyridine-7-carboxylic acid derivatives

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a Institute of Chemical Biology, Henan University, Kaifeng 475001, China;
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b Centre of Drug Discovery, China Pharmaceutical University, Nanjing 210009, China

Corresponding author: Guo-Qiang Hu,
Received Date: 4 July 2014
Available Online: 2 September 2014
Fund Project:

Novel tricyclic fluoroquinolones, [1,2,4]triazolo[3,4-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.
- Triazole,
- Tricyclic fluoroquinolone,
- Synthesis,
- Antibacterial activity
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沈阳化工大学材料科学与工程学院沈阳 110142