Structure-Activity Relationship for the Picolinamide Antibacterials that Selectively Target Clostridioides difficile.

ABSTRACT: Clostridioides difficile is a leading health threat. This pathogen initiates intestinal infections during gut microbiota dysbiosis caused by oral administration of antibiotics. C. difficile is difficult to eradicate due to its ability to form spores, which are not susceptible to antibiotics. To address the urgent need for treating recurrent C. difficile infection, antibiotics that selectively target C. difficile over common gut microbiota are needed. We herein describe the class of picolinamide antibacterials which show potent and selective activity against C. difficile. The structure-activity relationship of 108 analogues of isonicotinamide 4, a compound that is equally active against methicillin-resistant Staphylococcus aureus and C. di

SUBMITTER: Speri E 

PROVIDER: S-EPMC8201750 | biostudies-literature | 2021 Jun

REPOSITORIES: biostudies-literature