Antitrypanosomal and antileishmanial activities of novel N-alkyl-(1-phenylsubstituted-beta-carboline)-3-carboxamides.
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.
Tonin
Lilian T Düsman
LT
Departamento de Química, Universidade Estadual de Maringá, Avenida Colombo, 5790, Zona 7, 87020-900, Maringá, PR, Brazil.
Panice
Manuela Ribeiro
MR
Nakamura
Celso Vataru
CV
Rocha
Karin Juliane Pelizzaro
KJ
dos Santos
Adriana Oliveira
AO
Ueda-Nakamura
Tânia
T
da Costa
Willian Ferreira
WF
Sarragiotto
Maria Helena
MH
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*
D002243:Carbolines; D014344:Trypanocidal Agents