Screening for potent and selective anticlostridial leads among FDA-approved drugs.

ABSTRACT: Clostridium difficile is a leading cause of morbidity and mortality particularly in hospital settings. In addition, treatment is very challenging due to the scarcity of effective therapeutic options. Thus, there remains an unmet need to identify new therapeutic agents capable of treating C. difficile infections. In the current study, we screened two FDA-approved drug libraries against C. difficile. Out of almost 3200 drugs screened, 50 drugs were capable of inhibiting the growth of C. difficile. Remarkably, some of the potent inhibitors have never been reported before and showed activity in a clinically achievable range. Structure-activity relationship analysis of the active hits clustered the potent inhibitors into four chemical groups; nitroimidazoles (MIC₅₀ = 0.06-2.7 μM), sa

SUBMITTER: AbdelKhalek A 

PROVIDER: S-EPMC7211121 | biostudies-literature | 2020 Jun

REPOSITORIES: biostudies-literature