1-(substituted)benzyl-5-aminoimidazole-4-carboxamides are potent orally active inhibitors of Trypanosoma cruzi in mice.
1-(Substituted)benzyl-5-aminoimidazole-4-carboxamides are potent orally active inhibitors of Trypanosoma cruzi infections in mice. The most active compounds are the 1-(4-chlorobenzyl)- and 1-(3,4-dichlorobenzyl)-analogs (L-153,094 [2] and L-153,153 [4], resp.) which are approximately 7-fold more potent upon oral administration than nifurtimox (Lampit) in suppressing parasite levels in the blood of mice with acute Trypanosoma cruzi infections.
Chabala
J C
JC
Merck Sharp & Dohme Research Laboratories, Rahway, New Jersey 07065.
Waits
V B
VB
Ikeler
T
T
Patchett
A A
AA
Payne
L
L
Peterson
L H
LH
Reamer
R A
RA
Hoogsteen
K
K
Wyvratt
M
M
Hanson
W L
WL
D000620:Aminoimidazole Carboxamide / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000627:therapeutic use*; D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000627:therapeutic use*; D014355:Chagas Disease / Q000188:drug therapy*; D003198:Computer Simulation; D005260:Female; D051379:Mice; D008815:Mice, Inbred Strains; D008958:Models, Molecular; D008968:Molecular Conformation; D013329:Structure-Activity Relationship; D014349:Trypanosoma cruzi
D000981:Antiprotozoal Agents; D000620:Aminoimidazole Carboxamide