In:
ChemMedChem, Wiley, Vol. 15, No. 2 ( 2020-01-17), p. 210-218
Abstract:
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‐β 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 .
Type of Medium:
Online Resource
ISSN:
1860-7179
,
1860-7187
DOI:
10.1002/cmdc.201900560
Language:
English
Publisher:
Wiley
Publication Date:
2020
detail.hit.zdb_id:
2209649-8
SSG:
15,3
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