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ACS Chem Biol. 2014 May 16;9(5):1172-7. doi: 10.1021/cb500080r. Epub 2014 Mar 17.

Teaching 'old' polymyxins new tricks: new-generation lipopeptides targeting gram-negative 'superbugs'.

Author information

1
Drug Delivery, Disposition and Dynamics, ‡Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University , 381 Royal Parade, Parkville 3052, Victoria, Australia.

Abstract

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.

PMID:
24601489
PMCID:
PMC4033650
DOI:
10.1021/cb500080r
[Indexed for MEDLINE]
Free PMC Article
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