Effects of 3-chloro-phenyl-1,4-dihydropyridine derivatives on Trypanosome cruzi epimastigotes.
A series of 3-chloro-phenyl-1,4-dihydropyridine derivatives produced different degrees of inhibition of parasite growth and respiration on clone Brener, LQ and Tulahuen strains of Trypanosome cruzi epimastigotes. Respiratory chain inhibition appears to be a posible determinant of the trypanosomicidal activity of this compounds. No difference in the action of these derivatives was found among the different parasite strains. For comparative purposes, the inhibitory effects of felodipine and nicardipine are also reported. A good correlation between toxic effects and the easiness of oxidation of the dihydripyridine ring was found. The presence of a fused ring on the dihydropyridine moiety significantly diminished the inhibitory effects.
Maya
J D
JD
Program of Clinical and Molecular Pharmacology, Institute of Biomedical Sciences, Faculty of Medicine, University of Chile, PO Box 70086, Santiago, Chile.
Morello
A
A
Repetto
Y
Y
Tellez
R
R
Rodriguez
A
A
Zelada
U
U
Puebla
P
P
Caballero
E
E
Medarde
M
M
Núñez-Vergara
L J
LJ
Squella
J A
JA
Bontá
M
M
Bollo
S
S
San Feliciano
A
A
D000818:Animals; D002121:Calcium Channel Blockers / Q000494:pharmacology; D002465:Cell Movement / Q000187:drug effects; D004095:Dihydropyridines / Q000737:chemistry / Q000494:pharmacology*; D004563:Electrochemistry; D015736:Felodipine / Q000494:pharmacology; D009529:Nicardipine / Q000494:pharmacology; D010084:Oxidation-Reduction; D010101:Oxygen Consumption / Q000187:drug effects; D014344:Trypanocidal Agents / Q000737:chemistry / Q000494:pharmacology*; D014349:Trypanosoma cruzi / Q000187:drug effects* / Q000254:growth & development / Q000378:metabolism
D002121:Calcium Channel Blockers; D004095:Dihydropyridines; D014344:Trypanocidal Agents; D009529:Nicardipine; D015736:Felodipine