4.5 Article

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

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CHEMISTRY & BIODIVERSITY
卷 15, 期 10, 页码 -

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WILEY-V C H VERLAG GMBH
DOI: 10.1002/cbdv.201800261

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quinolone; ciprofloxacin; 1; 2; 4-triazole-5(4H)-thione; antibacterial activities; structure-activity relationship

资金

  1. NSFC [21502237]

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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 invitro 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.

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