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 for the identification of new potential Trypanosoma cruzi target(s).
Bonnet
B
B
Institut de Biologie et Institut Pasteur de Lille, UMR CNRS 8525, Faculté de Pharmacie, Université de Lille II, France.
Soullez
D
D
Girault
S
S
Maes
L
L
Landry
V
V
Davioud-Charvet
E
E
Sergheraert
C
C
D000818:Animals; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D009247:NADH, NADPH Oxidoreductases / Q000037:antagonists & inhibitors*; D010879:Piperazines / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000737:chemistry / Q000494:pharmacology*; D014349:Trypanosoma cruzi / Q000187:drug effects*
D010879:Piperazines; D014344:Trypanocidal Agents; D009247:NADH, NADPH Oxidoreductases; C049608:trypanothione reductase