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Design, Synthesis and Antibacterial Evaluation of 1‐[(1 R ,2 S )‐2‐Fluorocyclopropyl]ciprofloxacin‐1,2,4‐triazole‐5(4 H )‐thione Hybrids
Author(s) -
Gao Yang,
Na LuXin,
Xu Zhi,
Zhang Shu,
Wang APeng,
Lü Kai,
Guo HuiYuan,
Liu MingLiang
Publication year - 2018
Publication title -
chemistry and biodiversity
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.427
H-Index - 70
eISSN - 1612-1880
pISSN - 1612-1872
DOI - 10.1002/cbdv.201800261
Subject(s) - ciprofloxacin , chemistry , hybrid , triazole , gram , potency , levofloxacin , in vitro , antibacterial activity , stereochemistry , microbiology and biotechnology , combinatorial chemistry , antibiotics , bacteria , biology , organic chemistry , botany , genetics , biochemistry
A new class of 1‐[(1 R ,2 S )‐2‐fluorocyclopropyl]ciprofloxacin ( CPFX )‐1,2,4‐triazole‐5(4 H )‐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‐[(1 R ,2 S )‐2‐fluorocyclopropyl] CPFX ( 1 ) and comparable to CPFX and levofloxacin against the majority of the tested pathogens, worth to be further investigated.