Trypanocidal activity of 4 isopropyl salicylaldehyde and 4-isopropyl salicylic acid on Trypanosoma cruzi.
We synthesized and study the possible trypanocidal activity of 4-isopropyl salicylaldehyde and 4-isopropyl salicylic acid, these compounds were chemical derivatives of gossypol, a drug that inhibits the growth of T. cruzi in culture. These derivatives were tested in two T. cruzi strains with different in vitro susceptibility to benznidazole and nifurtimox, used as a reference drugs. It was found that they were better inhibitors of T. cruzi alpha-hydroxyacid dehydrogenase than gossypol, in both strains. The in vitro and in vivo pharmacological tests were performed and in both test, the gossypol derivatives showed a higher and better trypanocidal effect than gossypol, and a higher and much better trypanocidal effect than nifurtimox and benznidazole in the two studied T. cruzi strains. The trypanocidal effect was higher in the NINOA strain than in the MIGUZ strain.
Nogueda-Torres
B
B
Departamento de Bioquímica, Escuela Nacional de Ciencias Biológicas, Instituto Politécnico Nacional. Apdo. Postal 4-080, Admon. 4, México 06401 DF, México.
Rodríguez-Paez
L
L
Ramírez
I B
IB
Ramírez
C W
CW
D000429:Alcohol Oxidoreductases / Q000037:antagonists & inhibitors; D000447:Aldehydes / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D000818:Animals; D014355:Chagas Disease / Q000188:drug therapy; D004353:Drug Evaluation, Preclinical; D006072:Gossypol / Q000737:chemistry / Q000494:pharmacology; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D015394:Molecular Structure; D009547:Nifurtimox / Q000494:pharmacology; D009593:Nitroimidazoles / Q000494:pharmacology; D015800:Protozoan Proteins / Q000037:antagonists & inhibitors; D012459:Salicylates / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D014344:Trypanocidal Agents / Q000494:pharmacology* / Q000627:therapeutic use; D014349:Trypanosoma cruzi / Q000187:drug effects*
C519214:4-isopropyl salicylaldehyde; C519213:4-isopropyl salicylic acid; D000447:Aldehydes; D009593:Nitroimidazoles; D015800:Protozoan Proteins; D012459:Salicylates; D014344:Trypanocidal Agents; D000429:Alcohol Oxidoreductases; C021379:D-2-hydroxyacid dehydrogenase; D006072:Gossypol; D009547:Nifurtimox; C009999:benzonidazole