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Synthesis,Cytotoxicity and Antileishmanial Activity of Some N-(2-(indol-3-yl)ethyl)-7-chloroquinolin-4-amines
Authors:Elaine S Coimbra  Rafael Carvalhaes  Richard M Grazul  Patricia A Machado  Marcos V N De Souza  Adilson D Da Silva
Affiliation:1. Departamento de Parasitologia, Microbiologia e Imunologia, Instituto de Ciências Biológicas, Universidade Federal de Juiz de Fora, Juiz de Fora, M.G. 36036-900, Brasil;2. Departamento de Quimica, Instituto de Ciências Exatas, Universidade Federal de Juiz de Fora, Juiz de Fora, M.G. 36036-900, Brasil;3. FioCruz- Fundação Oswaldo Cruz, Instituto de Tecnologia em Fármacos-Far Manguinhos, Rua Sizenando Nabuco, 100, Manguinhos, Rio de Janeiro, R.J. 21041-250, Brasil
Abstract:We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3) . Hydrolysis of the methyl ester adduct (5) yielded the free acid (6) . The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.
Keywords:4  7  dichloroquinoline  7  chloroquinolin  4  amines  Leishmania  N  2  indol  3  yl  ethyl  7  chloroquinolin  4  amines  tryptamine  tryptophan
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