期刊
ACS CHEMICAL BIOLOGY
卷 9, 期 5, 页码 1172-1177出版社
AMER CHEMICAL SOC
DOI: 10.1021/cb500080r
关键词
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资金
- National Institute of Allergy and Infectious Diseases of the National Institutes of Health [R01AI098771]
- Australian National Health and Medical Research Council (NHMRC)
The antimicrobial lipopeptides polymyxin B and E (colistin) are being used as a 'last-line' therapy for infections caused by multidrug-resistant Gram-negative pathogens. Polymyxin resistance implies a total lack of antibiotics for the treatment of life-threatening infections caused by the Gram-negative 'superbugs'. This report details the structure-activity relationships (SAR) based design, in toto synthesis, and preclinical evaluation of a series of novel polymyxin lipopeptides with better antibacterial activity against polymyxin-resistant Gram-negative bacteria.
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