Trypanothione reductase inhibition/trypanocidal activity relationships in a 1,4-bis(3-aminopropyl)piperazine series

B Bonnet; D Soullez; S Girault; L Maes; V Landry; E Davioud-Charvet; C Sergheraert

doi:10.1016/s0968-0896(99)00268-0

Trypanothione reductase inhibition/trypanocidal activity relationships in a 1,4-bis(3-aminopropyl)piperazine series

Bioorg Med Chem. 2000 Jan;8(1):95-103. doi: 10.1016/s0968-0896(99)00268-0.

Authors

B Bonnet¹, D Soullez, S Girault, L Maes, V Landry, E Davioud-Charvet, C Sergheraert

Affiliation

¹ Institut de Biologie et Institut Pasteur de Lille, UMR CNRS 8525, Faculté de Pharmacie, Université de Lille II, France.

PMID: 10968268
DOI: 10.1016/s0968-0896(99)00268-0

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).

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Cell Line
Cell Survival / drug effects
Humans
Magnetic Resonance Spectroscopy
NADH, NADPH Oxidoreductases / antagonists & inhibitors*
Piperazines / chemistry
Piperazines / pharmacology*
Structure-Activity Relationship
Trypanocidal Agents / chemistry
Trypanocidal Agents / pharmacology*
Trypanosoma cruzi / drug effects*

Substances

Piperazines
Trypanocidal Agents
NADH, NADPH Oxidoreductases
trypanothione reductase