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

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.

SUBMITTER: Velkov T

PROVIDER: S-EPMC4033650 | biostudies-literature | 2014 May

REPOSITORIES: biostudies-literature

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

Velkov Tony T Roberts Kade D KD Nation Roger L RL Wang Jiping J Thompson Philip E PE Li Jian J

ACS chemical biology 20140317 5

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 anti ...[more]

PMID: 24601489

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