1.
Bioorg Med Chem
; 8(1): 95-103, 2000 Jan.
Article
in English
| MEDLINE
| ID: mdl-10968268
ABSTRACT
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).
Subject(s)
NADH, NADPH Oxidoreductases/antagonists & inhibitors , Piperazines/pharmacology , Trypanocidal Agents/pharmacology , Trypanosoma cruzi/drug effects , Animals , Cell Line , Cell Survival/drug effects , Humans , Magnetic Resonance Spectroscopy , Piperazines/chemistry , Structure-Activity Relationship , Trypanocidal Agents/chemistry
2.
Bioorg Med Chem
; 5(7): 1249-56, 1997 Jul.
Article
in English
| MEDLINE
| ID: mdl-9377084
ABSTRACT
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.
