Journal
CHEMMEDCHEM
Volume 15, Issue 2, Pages 210-218Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.201900560
Keywords
antibiotic resistance; adjuvants; colistin; Gram-negative bacteria
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Funding
- US National Institutes of Health (NIH) [1R01AI136904]
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Infections caused by multidrug-resistant (MDR) bacteria, particularly Gram-negative bacteria, are an escalating global health threat. Often clinicians are forced to administer the last-resort antibiotic colistin; however, colistin resistance is becoming increasingly prevalent, giving rise to the potential for a situation in which there are no treatment options for MDR Gram-negative infections. The development of adjuvants that circumvent bacterial resistance mechanisms is a promising orthogonal approach to the development of new antibiotics. We recently disclosed that the known IKK-beta inhibitor IMD-0354 potently suppresses colistin resistance in several Gram-negative strains. In this study, we explore the structure-activity relationship (SAR) between the IMD-0354 scaffold and colistin resistance suppression, and identify several compounds with more potent activity than the parent against highly colistin-resistant strains of Acinetobacter baumannii and Klebsiella pneumoniae.
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