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.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6892603 | PMC |
| http://dx.doi.org/10.1016/j.bmcl.2019.126778 | DOI Listing |
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