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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. Copyright © 2019 Elsevier Ltd. All rights reserved.

Citation

Xiaofang Wang, Monica Cal, Marcel Kaiser, Frederick S Buckner, Galina I Lepesheva, Austin G Sanford, Alexander I Wallick, Paul H Davis, Jonathan L Vennerstrom. A new chemotype with promise against Trypanosoma cruzi. Bioorganic & medicinal chemistry letters. 2020 Jan 01;30(1):126778

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PMID: 31706668

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