title: Novel 1,3,4-thiadiazolium-2-phenylamine chlorides derived from natural piperine as trypanocidal agents: chemical and biological studies.
abstract: We herein describe the synthesis and characterization of nine new 1,3,4-thiadiazolium-2-phenylamine chlorides derived from natural piperine. We evaluate their toxic effects against the different evolutive forms of Trypanosoma cruzi, and the host cell (murine macrophages). The results obtained show that mesoionic hydrochloride MI possesses the best activity profile. Compound MI may be a prototype for use in the development of a new chemotherapeutic agent with high efficiency, which may be employed in the treatment of Chagas' disease.
authors.affiliation: Universidade Federal Rural do Rio de Janeiro, Instituto de Ciências Exatas, Departamento de Química, Rodovia BR 465, Km 7, CEP 23.890-000 Seropédica, RJ, Brazil.
authors.forename: Welisson
authors.initials: W
authors.lastname: da Silva Ferreira
authors.forename: Leonardo
authors.initials: L
authors.lastname: Freire-de-Lima
authors.forename: Víctor Barbosa
authors.initials: VB
authors.lastname: Saraiva
authors.forename: Frederico
authors.initials: F
authors.lastname: Alisson-Silva
authors.forename: Lucia
authors.initials: L
authors.lastname: Mendonça-Previato
authors.forename: José Osvaldo
authors.initials: JO
authors.lastname: Previato
authors.forename: Aurea
authors.initials: A
authors.lastname: Echevarria
authors.forename: Marco Edilson Freire
authors.initials: ME
authors.lastname: de Lima
mesh_terms: D000470:Alkaloids / Q000737:chemistry* / Q000494:pharmacology*; D000818:Animals; D052117:Benzodioxoles / Q000737:chemistry* / Q000494:pharmacology*; D014355:Chagas Disease / Q000188:drug therapy; D008264:Macrophages / Q000469:parasitology; D051379:Mice; D010880:Piperidines / Q000737:chemistry* / Q000494:pharmacology*; D053284:Polyunsaturated Alkamides / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000737:chemistry*; D014349:Trypanosoma cruzi / Q000187:drug effects
chemical_list: D000470:Alkaloids; D052117:Benzodioxoles; D010880:Piperidines; D053284:Polyunsaturated Alkamides; D014344:Trypanocidal Agents; C008922:piperine