Potent kinase inhibitors from the Merck KGaA OGHL: Novel hits against Trypanosoma brucei with potential for repurposing.

ABSTRACT: African trypanosomiasis remains a critical public health concern, with over 55 million people still at risk of infection. There are several issues associated with the current therapies including toxicity and resistance, which represent the main bottleneck of trypanosomiasis control. Thus, it is urgent to develop novel therapeutic tools with distinct mechanisms of action. The in vitro phenotypic screening of the Merck KGaA Darmstadt German Open Global Health Library (OGHL) against Trypanosoma brucei brucei yielded three potent kinase inhibitors belonging to different chemical series: a phenylcarbonylacrylamide (OGHL00006); a 2,4-di(phenylamino)pyrimidine (OGHL00133); and a 3-(triazol-4-yl)-7-azaindole (OGHL00169). They exhibited low micromolar to nanomolar median inhibitory concentrations (

SUBMITTER: Dize D 

PROVIDER: S-EPMC12622802 | biostudies-literature | 2025 Nov

REPOSITORIES: biostudies-literature