title: Anti-Trichomonas vaginalis activity of synthetic lipophilic diamine and amino alcohol derivatives.
abstract: Taking in account the increased prevalence of metronidazole-resistant infections, alternative drugs are necessary for the treatment of trichomonosis. We report in this work the preparation and the in vitro anti-trichomonads activity of two diamines 1 and 2, and three different lipophilic amino alcohol derivatives 3, 4 and 5. These compounds were tested for in vitro activity against two isolates of Trichomonas vaginalis and displayed inhibition of the parasite growth. Five concentrations of each compound were tested. The butanediamine derivative 1, at a final concentration of 5.85 microM, presented a cytotoxic effect against 47% of T. vaginalis trophozoites. Furthermore, the cytotoxicity of 1 did not present statistically significant difference when compared to metronidazole in the same range of concentration (0.1-1.5 microg/mL).
authors.affiliation: Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Av. Ipiranga 2752, 90610-000 Porto Alegre, RS, Brazil.
authors.forename: Raquel B
authors.initials: RB
authors.lastname: Giordani
authors.forename: Mauro V
authors.initials: MV
authors.lastname: De Almeida
authors.forename: Ederson
authors.initials: E
authors.lastname: Fernandes
authors.forename: Cristiane
authors.initials: C
authors.lastname: França da Costa
authors.forename: Geraldo A
authors.initials: GA
authors.lastname: De Carli
authors.forename: Tiana
authors.initials: T
authors.lastname: Tasca
authors.forename: José A S
authors.initials: JA
authors.lastname: Zuanazzi
mesh_terms: D000605:Amino Alcohols / Q000138:chemical synthesis / Q000494:pharmacology*; D000994:Antitrichomonal Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D003959:Diamines / Q000138:chemical synthesis / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D013329:Structure-Activity Relationship; D014246:Trichomonas vaginalis / Q000187:drug effects* / Q000254:growth & development
chemical_list: D000605:Amino Alcohols; D000994:Antitrichomonal Agents; D003959:Diamines