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  • 标题:Synthesis and Antimicrobial Activity of 2-Trifluoroacetonylbenzoxazole Ligands and Their Metal Complexes
  • 本地全文:下载
  • 作者:Genki Watanabe ; Hiroshi Sekiya ; Eiji Tamai
  • 期刊名称:Chemical and Pharmaceutical Bulletin
  • 印刷版ISSN:0009-2363
  • 电子版ISSN:1347-5223
  • 出版年度:2018
  • 卷号:66
  • 期号:7
  • 页码:732-740
  • DOI:10.1248/cpb.c18-00158
  • 语种:English
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:Three 2-fluoroacetonylbenzoxazole ligands 1a – c and their new Zn(II) complexes 2a – c have been synthesized. In addition, syntheses of new metal [Mg(II), Ni(II), Cu(II), Pd(II), and Ag(I)] complexes from 1a have been also described. The molecular and crystal structures of six metal complexes 2b and 2d – h were determined by single-crystal X-ray diffraction analyses. Their antibacterial activities against six Gram-positive and six Gram-negative bacteria were evaluated by minimum inhibitory concentrations (MIC), which were compared with those of appropriate antibiotics and silver nitrate. The results indicate that some metal compounds have more antibacterial effects in comparison with free ligands and have preferred antibacterial activities that may have potential pharmaceutical applications. Noticeably, the Ag(I) complex 2h exhibited low MIC value of 0.7 µM against Pseudomonas aeruginosa , which was even superior to the reference drug, Norfloxacin with that of 1.5 µM. Against P. aeruginosa , 2h is bacteriostatic, exerts the cell surface damage observed by scanning electron microscopy (SEM) and is less likely to develop resistance. The new 2h has been found to display effective antimicrobial activity against a series of bacteria.
  • 关键词:antibacterial activity;fluorinated benzoxazole;metal complex;trifluoroacetyl
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