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

Autor: 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.; HuangHuai University, Zhumadian 463000, P. R. China., Zhang S; Pony Testing International Group Co. Ltd. (Wuhan), Wuhan 430034, P. R. China., Wang AP; Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, 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.
Jazyk: angličtina
Zdroj: Chemistry & biodiversity [Chem Biodivers] 2018 Oct; Vol. 15 (10), pp. e1800261. Date of Electronic Publication: 2018 Oct 09.
DOI: 10.1002/cbdv.201800261
Abstrakt: 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.
(© 2018 Wiley-VHCA AG, Zurich, Switzerland.)
Databáze: MEDLINE
Externí odkaz: