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Design, Synthesis and Antibacterial Evaluation of 1-[(1R,2S)-2-Fluorocyclopropyl]ciprofloxacin-1,2,4-triazole-5(4H)-thione Hybrids.
Gao, Yang; Na, Lu-Xin; Xu, Zhi; Zhang, Shu; Wang, A-Peng; Lü, Kai; Guo, Hui-Yuan; Liu, Ming-Liang.
Afiliação
  • Gao Y; Xuanwu Hospital, Capital Medical University, Beijing, 100053, P. R. China.
  • Na LX; Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, P. R. China.
  • Xu Z; Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, P. R. China.
  • Zhang S; HuangHuai University, Zhumadian 463000, P. R. China.
  • Wang AP; Pony Testing International Group Co. Ltd. (Wuhan), Wuhan 430034, P. R. China.
  • Lü K; Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, P. R. China.
  • Guo HY; Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, P. R. China.
  • Liu ML; Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, P. R. China.
Chem Biodivers ; 15(10): e1800261, 2018 Oct.
Article em En | MEDLINE | ID: mdl-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.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Triazóis / Desenho de Fármacos / Ciprofloxacina / Antibacterianos Limite: Humans Idioma: En Revista: Chem Biodivers Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2018 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Triazóis / Desenho de Fármacos / Ciprofloxacina / Antibacterianos Limite: Humans Idioma: En Revista: Chem Biodivers Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2018 Tipo de documento: Article