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A new chemotype with promise against Trypanosoma cruzi.
Wang, Xiaofang; Cal, Monica; Kaiser, Marcel; Buckner, Frederick S; Lepesheva, Galina I; Sanford, Austin G; Wallick, Alexander I; Davis, Paul H; Vennerstrom, Jonathan L.
Afiliación
  • Wang X; College of Pharmacy, University of Nebraska Medical Center, 986025 Nebraska Medical Center, Omaha, NE, United States.
  • Cal M; Department of Medical Parasitology and Infection Biology, Swiss Tropical Institute, Socinstrasse 57, CH-4002 Basel, Switzerland; University of Basel, CH-4003 Basel, Switzerland.
  • Kaiser M; Department of Medical Parasitology and Infection Biology, Swiss Tropical Institute, Socinstrasse 57, CH-4002 Basel, Switzerland; University of Basel, CH-4003 Basel, Switzerland.
  • Buckner FS; Department of Medicine, University of Washington, 750 Republican Street, Seattle, WA, United States.
  • Lepesheva GI; Department of Biochemistry, Vanderbilt University, 2200 Pierce Ave., Nashville, TN, United States.
  • Sanford AG; Department of Biology, University of Nebraska at Omaha, Omaha, NE, United States.
  • Wallick AI; Department of Biology, University of Nebraska at Omaha, Omaha, NE, United States.
  • Davis PH; Department of Biology, University of Nebraska at Omaha, Omaha, NE, United States.
  • Vennerstrom JL; College of Pharmacy, University of Nebraska Medical Center, 986025 Nebraska Medical Center, Omaha, NE, United States. Electronic address: jvenners@unmc.edu.
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.
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Tripanocidas / Trypanosoma cruzi / Enfermedad de Chagas Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2020 Tipo del documento: Article País de afiliación: Estados Unidos
Texto completo
Imprimir
XML
PubMed Links
Buscar en Google

Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Tripanocidas / Trypanosoma cruzi / Enfermedad de Chagas Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2020 Tipo del documento: Article País de afiliación: Estados Unidos