Heterocyclic core modifications in trypanosomacidal 2-[(phenylheteroaryl)ethyl]ureas.

ABSTRACT: The protozoan parasites Trypanosoma brucei and Trypanosoma cruzi, which cause human African trypanosomiasis (HAT) and Chagas disease, respectively, are responsible for considerable human suffering. Reduced case numbers and improved treatment options for HAT provide hope, but the outlook for Chagas disease is less promising, and safer, more efficacious chemotherapy is sorely needed. We previously reported the discovery and optimisation of a novel class of potent and selective trypanosomacidal 2-[(2-phenylthiazolyl)ethyl]ureas active against both T. brucei brucei and T. cruzi. In the current work, replacement of the core thiazole with alternative heterocycles has revealed that a contiguous arrangement of phenyl substituent, hydrogen-bond-accepting nitrogen, and al

SUBMITTER: Toynton A 

PROVIDER: S-EPMC11832035 | biostudies-literature | 2025 Jan

REPOSITORIES: biostudies-literature