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1-[(1R,2S)-2-氟环丙基]环丙沙星-1,2,4-三唑-5(4H)-硫酮杂合物的设计、合成及抗菌活性评价

Design, Synthesis and Antibacterial Evaluation of 1-[(1R,2S)-2-Fluorocyclopropyl]ciprofloxacin-1,2,4-triazole-5(4H)-thione Hybrids.

作者信息

Gao Yang, Na Lu-Xin, Xu Zhi, Zhang Shu, Wang A-Peng, Lü Kai, Guo Hui-Yuan, Liu Ming-Liang

机构信息

Xuanwu Hospital, Capital Medical University, Beijing, 100053, P. R. China.

Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, P. R. China.

出版信息

Chem Biodivers. 2018 Oct;15(10):e1800261. doi: 10.1002/cbdv.201800261. Epub 2018 Oct 9.

DOI:10.1002/cbdv.201800261
PMID:29987907
Abstract

A new class of 1-[(1R,2S)-2-fluorocyclopropyl]ciprofloxacin (CPFX)-1,2,4-triazole-5(4H)-thione hybrids 6a - 6o was designed, synthesized and evaluated for their in vitro antibacterial activities against a panel of clinically important drug-sensitive and drug-resistant Gram-positive and Gram-negative pathogens. Our results revealed that all hybrids 6a - 6o had great potency against the tested strains, especially Gram-negative pathogens. The synthesized hybrids were more potent than the parent 1-[(1R,2S)-2-fluorocyclopropyl]CPFX (1) and comparable to CPFX and levofloxacin against the majority of the tested pathogens, worth to be further investigated.

摘要

设计、合成了一类新型的1-[(1R,2S)-2-氟环丙基]环丙沙星（CPFX）-1,2,4-三唑-5(4H)-硫酮杂合物6a - 6o，并评估了它们对一系列临床上重要的药敏和耐药革兰氏阳性及革兰氏阴性病原体的体外抗菌活性。我们的结果表明，所有杂合物6a - 6o对测试菌株均具有很强的活性，尤其是对革兰氏阴性病原体。合成的杂合物比母体1-[(1R,2S)-2-氟环丙基]CPFX（1）更具活性，并且在大多数测试病原体方面与环丙沙星和左氧氟沙星相当，值得进一步研究。

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