ID: ALA4342427
Journal: Bioorg Med Chem Lett
Title: A new chemotype with promise against Trypanosoma cruzi.
Authors: Wang X, Cal M, Kaiser M, Buckner FS, Lepesheva GI, Sanford AG, Wallick AI, Davis PH, Vennerstrom JL.
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.
CiteXplore: 31706668
DOI: 10.1016/j.bmcl.2019.126778
Patent ID: ┄