1.
Bioorg Med Chem
; 8(1): 95-103, 2000 Jan.
Artigo
em Inglês
| MEDLINE
| ID: mdl-10968268
RESUMO
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).
Assuntos
NADH NADPH Oxirredutases/antagonistas & inibidores , Piperazinas/farmacologia , Tripanossomicidas/farmacologia , Trypanosoma cruzi/efeitos dos fármacos , Animais , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Humanos , Espectroscopia de Ressonância Magnética , Piperazinas/química , Relação Estrutura-Atividade , Tripanossomicidas/química
2.
Bioorg Med Chem
; 5(7): 1249-56, 1997 Jul.
Artigo
em Inglês
| MEDLINE
| ID: mdl-9377084
RESUMO
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.
