In vitro activity of thienyl-2-nitropropene compounds against Trypanosoma cruzi.
The in vitro activity of four 2-nitropropene derivatives, 1-(3-benzothienyl)-2-nitropropene (N1), 1-(3-thienyl)-2-nitropropene (N2), 1-(5-bromo-2-thienyl)-2-nitropropene (N3) and 1-(4-bromo-2-thienyl)-2-nitropropene (N4), were tested against cultures of the parasite Trypanosoma cruzi. Cytotoxicity studies were performed using Vero cells. The blood trypomastigotes, amastigotes and epimastigotes showed differential degrees of sensitivity towards the four tested compounds; the highest activity against the epimastigotes and blood tripomastigotes was exhibited by N1, followed by N3, N4 and finally N2. In contrast, whereas the compounds N1, N3 and N4 exerted similar magnitudes of activity against amastigotes, N2 was found to be a much less potent compound. According to our results, the compound N1 had the highest level of activity (IC50: 0.6 microM) against epimastigotes.
Herrera
Cristina
C
Instituto de Investigaciones Farmacéuticas, Facultad de Farmacia, Universidad de Costa Rica, San José, Costa Rica. cristina.herrera@ucr.ac.cr
Vallejos
Gabriel A
GA
Loaiza
Randall
R
Zeledón
Rodrigo
R
Urbina
Andrea
A
Sepúlveda-Boza
Silvia
S
D000704:Analysis of Variance; D000818:Animals; D000981:Antiprotozoal Agents / Q000494:pharmacology*; D002522:Chlorocebus aethiops; D009574:Nitro Compounds / Q000494:pharmacology*; D011721:Pyrenes / Q000494:pharmacology; D014349:Trypanosoma cruzi / Q000187:drug effects* / Q000254:growth & development; D014709:Vero Cells
D000981:Antiprotozoal Agents; D009574:Nitro Compounds; D011721:Pyrenes; C049029:2-nitropyrene