The efficacy of a novel compound, (E)-1-(4′-bromo-4-biphenylyl)-1-(4-chlorophenyl)-3-dimethylaminoprop-1-ene againstTrypanosoma cruzi in mice

Abstract

The biological properties of a novel compound 353C with high activity against Trypanosoma cruzi, are described. The compound was about 10 times and 20 times more effective than either benznidazole or nifurtimox respectively, in producing radical cure in mice. 353C has a long half-life and showed anti-trypanosomal properties when given to mice at weekly intervals.

5-Nitrofuranes and 5-nitrothiophenes with anti-Trypanosoma cruzi activity and ability to accumulate squalene

“…1) showed excellent in vitro anti-T. cruzi profile 33 and in vivo for some assayed Bppa derivatives. [33][34][35] In this sense, recently our group have described a series of 5-nitrofuranes able to accumulate squalene, and potentially inhibit SE, in T. cruzi parasite. 18 These nitrofuranes (1-4, Fig.…”

Experimental chemotherapy for Chagas disease: 15 years of research contributions from in vivo and in vitro studies

“…These compounds can easily penetrate the plasma membrane and accumulate in the lysosomes, where they become trapped in the protonised form as a result of the acid environment inside this organelle (Lüllmann et al 1978). Barrett et al (1982) have previously reported that the chloro derivative (X = Cl) tested as an E isomer salt is highly effective in suppressing mice infections induced by different stocks of T. cruzi and is more active than either Nf or Bz.…”

Trypanocidal activity of 2-propen-1-amine derivatives on trypomastigotes culture and in animal model

“…Discussion 2-Propen-1-amine derivatives possess a remarkable trypanocidal activity in vitro (De Conti et al 1996a and in vivo (Barrett et al 1982;Pereira et al 1998). However, the effect of each isolated isomer on this activity has not been examined before.…”