Selective activity of 2,4-diaryl-1,2,3,4-tetrahydroquinolines on Trypanosoma cruzi epimastigotes and amastigotes expressing β-galactosidase

The growth inhibitory effect on Trypanosoma cruzi epimastigotes and the unspecific cytotoxicity over NCTC-929 fibroblasts of two series of previously synthesized 2,4-diaryl-1,2,3,4-tetrahydroquinolines (THQ), have been studied in vitro and compared with those of benznidazole (BZ). Derivatives AR39,...

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Autores:
Tipo de recurso:
Fecha de publicación:
2013
Institución:
Ministerio de Ciencia, Tecnología e Innovación
Repositorio:
Repositorio Minciencias
Idioma:
eng
OAI Identifier:
oai:repositorio.minciencias.gov.co:20.500.14143/34187
Acceso en línea:
http://repositorio.colciencias.gov.co/handle/11146/34187
Palabra clave:
Plantas medicinales
Trypanosoma cruzi
Productos químicos
Trypanosoma cruzi
Tetrahydroquinolines
Cytotoxicity
Lipinski’s rule
OSIRIS software
Bioquímica vegetal
Aceites esenciales
Bioquímica vegetal
Tecnología química
Rights
License
http://purl.org/coar/access_right/c_f1cf
Description
Summary:The growth inhibitory effect on Trypanosoma cruzi epimastigotes and the unspecific cytotoxicity over NCTC-929 fibroblasts of two series of previously synthesized 2,4-diaryl-1,2,3,4-tetrahydroquinolines (THQ), have been studied in vitro and compared with those of benznidazole (BZ). Derivatives AR39, AR40, AR41, AR91 and DM15 achieved outstanding selectivity indexes (SI) on the extracellular form (SITHQ > SIBZ > 9.44) and thus, were tested in a more specific in vitro assay against amastigotes, showing less effectiveness than the reference drug (SIBZ > 320) but also accomplishing great selectivity on the intracellular stage (SITHQ > 25). These promising results, supported by the in-silico prediction of high bioavailability and less potential risk than benznidazole, reveal several tetrahydroquinolines as prototypes of potential antichagasic drugs.