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

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 f...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2000, Vol.8 (1), p.95-103
Hauptverfasser:	BONNET, B, SOULLEZ, D, GIRAULT, S, MAES, L, LANDRY, V, DAVIOUD-CHARVET, E, SERGHERAERT, A. C
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antibiotics. Antiinfectious agents. Antiparasitic agents Antiparasitic agents Biological and medical sciences Cell Line Cell Survival - drug effects Humans Magnetic Resonance Spectroscopy Medical sciences NADH, NADPH Oxidoreductases - antagonists & inhibitors Pharmacology. Drug treatments Piperazines - chemistry Piperazines - pharmacology Structure-Activity Relationship Trypanocidal Agents - chemistry Trypanocidal Agents - pharmacology Trypanosoma cruzi - drug effects
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Zusammenfassung:	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).
ISSN:	0968-0896 1464-3391
DOI:	10.1016/s0968-0896(99)00268-0