title: Antitrypanosomal and antileishmanial activities of novel N-alkyl-(1-phenylsubstituted-beta-carboline)-3-carboxamides.
abstract: A series of 1-phenylsubstituted beta-carbolines containing an N-butylcarboxamide group at C-3 of beta-carboline nucleus were synthesized and evaluated in vitro against epimastigote form of Trypanosoma cruzi and promastigote form of Leishmania amazonensis. Among all compounds tested, two derivatives (2b and 2d) presented potent activity against both parasites. The most active derivative 2b showed also the higher selectivity index ratio (SI) for L. amazonensis (SI=2,084). The effect of other N-alkylcarboxamide groups at C-3, such as pyrrolidyl, N-cyclohexil and N-benzylcarboxamide on T. cruzi and L. amazonensis activity was also evaluated. Our results pointed the synthesized beta-carboline-3-carboxamide derivatives as potential compounds for new drugs for Chagas' disease and leishmaniasis' treatment.
authors.affiliation: Departamento de Química, Universidade Estadual de Maringá, Avenida Colombo, 5790, Zona 7, 87020-900, Maringá, PR, Brazil.
authors.forename: Lilian T Düsman
authors.initials: LT
authors.lastname: Tonin
authors.forename: Manuela Ribeiro
authors.initials: MR
authors.lastname: Panice
authors.forename: Celso Vataru
authors.initials: CV
authors.lastname: Nakamura
authors.forename: Karin Juliane Pelizzaro
authors.initials: KJ
authors.lastname: Rocha
authors.forename: Adriana Oliveira
authors.initials: AO
authors.lastname: dos Santos
authors.forename: Tânia
authors.initials: T
authors.lastname: Ueda-Nakamura
authors.forename: Willian Ferreira
authors.initials: WF
authors.lastname: da Costa
authors.forename: Maria Helena
authors.initials: MH
authors.lastname: Sarragiotto
mesh_terms: D000818:Animals; D002243:Carbolines / Q000138:chemical synthesis / Q000494:pharmacology*; D007894:Leishmania mexicana / Q000187:drug effects*; D051379:Mice; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D014349:Trypanosoma cruzi / Q000187:drug effects*
chemical_list: D002243:Carbolines; D014344:Trypanocidal Agents