Teaching ‘Old’ Polymyxins New Tricks: New-Generation Lipopeptides Targeting Gram-Negative ‘Superbugs’ | Zendy

Tony Velkov | Zendy; Kade D. Roberts | Zendy; Roger L. Nation | Zendy; Jiping Wang | Zendy; Philip E. Thompson | Zendy; Jian Li | Zendy

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Teaching ‘Old’ Polymyxins New Tricks: New-Generation Lipopeptides Targeting Gram-Negative ‘Superbugs’

Author(s) -

Tony Velkov,

Kade D. Roberts,

Roger L. Nation,

Jiping Wang,

Philip E. Thompson,

Jian Li

Publication year - 2014

Publication title -

acs chemical biology

Language(s) - Uncategorized

Resource type - Journals

SCImago Journal Rank - 1.899

H-Index - 111

eISSN - 1554-8937

pISSN - 1554-8929

DOI - 10.1021/cb500080r

Subject(s) - polymyxin , colistin , polymyxin b , microbiology and biotechnology , antibiotics , antimicrobial , gram negative bacteria , gram , biology , bacteria , escherichia coli , biochemistry , genetics , gene

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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