Multidrug-resistant bacterial infections have become a global threat. We recently disclosed that the known IKK-β inhibitor IMD-0354 and subsequent analogues abrogate colistin resistance in several Gram-negative strains. Herein, we report the activity of a second-generation library of IMD-0354 analogues incorporating a benzimidazole moiety as an amide isostere. We identified several analogues that show increased colistin potentiation activity against Gram-negative bacteria.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8958665PMC
http://dx.doi.org/10.1021/acsinfecdis.1c00463DOI Listing

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