1.
Bioorg Med Chem
; 8(1): 95-103, 2000 Jan.
Artículo
en Inglés
| MEDLINE
| ID: mdl-10968268
RESUMEN
A series of symmetrically substituted 1,4-bis(3-aminopropyl)piperazines was synthesized and tested towards trypanothione reductase and for its in vitro trypanocidal potency. The most trypanocidal amongst them was found to be totally inactive towards the enzyme and thus constitutes a lead structure for the identification of new potential Trypanosoma cruzi target(s).
Asunto(s)
NADH NADPH Oxidorreductasas/antagonistas & inhibidores , Piperazinas/farmacología , Tripanocidas/farmacología , Trypanosoma cruzi/efectos de los fármacos , Animales , Línea Celular , Supervivencia Celular/efectos de los fármacos , Humanos , Espectroscopía de Resonancia Magnética , Piperazinas/química , Relación Estructura-Actividad , Tripanocidas/química
2.
Bioorg Med Chem
; 5(7): 1249-56, 1997 Jul.
Artículo
en Inglés
| MEDLINE
| ID: mdl-9377084
RESUMEN
Several spermine and spermidine derivatives containing 2-amino diphenylsulfide substituents were prepared and tested for their inhibiting effects on Trypanosoma cruzi trypanothione reductase. IC50 values were assessed between 0.3 and 3 microM. Compound 32 (Ki = 0.4 microM) is the most potent TR inhibitor described so far.