A new chemotype with promise against Trypanosoma cruzi. Issue 1 (1st January 2020) - Wang, Xiaofang
Graphical abstract: 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.