Journal
CHINESE CHEMICAL LETTERS
Volume 26, Issue 1, Pages 149-151Publisher
ELSEVIER SCIENCE INC
DOI: 10.1016/j.cclet.2014.09.017
Keywords
Triazole; Tricyclic fluoroquinolone; Synthesis; Antibacterial activity
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Funding
- National Natural Science Foundation of China [20872028, 21072045]
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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 mu g/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. (C) 2014 Guo-Qiang Hu. Published by Elsevier B.V. on behalf of Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. All rights reserved.
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