A new chemotype with promise against Trypanosoma cruzi.

ABSTRACT: Pyridyl benzamide 2 is a potent inhibitor of Trypanosoma cruzi, but not other protozoan parasites, and had a selectivity-index of ≥10. The initial structure-activity relationship (SAR) indicates that benzamide and sulfonamide functional groups, and N-methylpiperazine and sterically unhindered 3-pyridyl substructures are required for high activity against T. cruzi. Compound 2 and its active analogs had low to moderate metabolic stabilities in human and mouse liver microsomes.

SUBMITTER: Wang X 

PROVIDER: S-EPMC6892603 | biostudies-literature | 2020 Jan

REPOSITORIES: biostudies-literature