期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 178, 期 -, 页码 500-514出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2019.05.087
关键词
Antimicrobial resistance; ESKAPE bacteria; Drug resistance; Pyrrole; DNA gyrase
资金
- EPSRC (Global Challenges Competition King's College London)
- Royal Society [RG160870]
- University of London
- University of Rome [2682]
Antibiotic resistance represents a major threat worldwide. Gram-positive and Gram-negative opportunistic pathogens are becoming resistant to all known drugs mainly because of the overuse and misuse of these medications and the lack of new antibiotic development by the pharmaceutical industry. There is an urgent need to discover structurally innovative antibacterial agents for which no pre-existing resistance is known. This work describes the identification, synthesis and biological evaluation of a novel series of 1,5-diphenylpyrrole compounds active against a panel of ESKAPE bacteria. The new compounds show high activity against both wild type and drug-resistant Gram + ve and Gram-ve pathogens at concentrations similar or lower than levofloxacin. Microbiology studies revealed that the plausible target of the pyrrole derivatives is the bacterial DNA gyrase, with the pyrrole derivatives displaying similar inhibitory activity to levofloxacin against the wild type enzyme and retaining activity against the fluoroquinolone-resistant enzyme. (C) 2019 Elsevier Masson SAS. All rights reserved.
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