Dehydrodieugenol B derivatives as antiparasitic agents: Synthesis and biological activity against Trypanosoma cruzi
European Journal of Medicinal Chemistry
;
1762019.
Artículo
en Portugués
| LILACS, SES-SP, SESSP-IALPROD, SES-SP, SESSP-IALACERVO
| ID: biblio-1007421
ABSTRACT
Chagas disease is a neglected protozoan disease that affects more than eight million people in developing countries. Due to the limited number and toxicity proï¬les of therapies in current use, new drugs are urgently needed. In previous studies, we reported the isolation of two related antitrypanosomal neo- lignans from Nectandra leucantha (Lauraceae). In this work, a semi-synthetic library of twenty-three neolignan derivatives was prepared to explore synthetically accessible structure activity relationships (SAR) against Trypanosoma cruzi. Five compounds demonstrated activity against trypomastigotes (IC50 values from 8 to 64 mM) and eight showed activity against intracellular amastigotes (IC50 values from 7 to 16 mM). Eighteen derivatives demonstrated no mammalian cytotoxicity up to 200 mM. The phenolic ac- etate derivative of natural dehydrodieugenol
Texto completo:
Disponible
Índice:
LILACS (Américas)
Asunto principal:
Trypanosoma cruzi
/
Enfermedad
/
Enfermedad de Chagas
Idioma:
Portugués
Revista:
European Journal of Medicinal Chemistry
Año:
2019
Tipo del documento:
Artículo
Institución/País de afiliación:
Secretaria da Saúde do Estado de São Paulo/BR
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