A new chemotype with promise against Trypanosoma cruzi.
Bioorg Med Chem Lett
; 30(1): 126778, 2020 01 01.
Article
en En
| MEDLINE
| ID: mdl-31706668
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.
Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Tripanocidas
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Trypanosoma cruzi
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Enfermedad de Chagas
Límite:
Animals
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Humans
Idioma:
En
Año:
2020
Tipo del documento:
Article