Dehydrodieugenol B derivatives as antiparasitic agents: Synthesis and biological activity against Trypanosoma cruzi
European Journal of Medicinal Chemistry
;
1762019.
Article
in Portuguese
| 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
Full text:
Available
Index:
LILACS (Americas)
Main subject:
Trypanosoma cruzi
/
Disease
/
Chagas Disease
Language:
Portuguese
Journal:
European Journal of Medicinal Chemistry
Year:
2019
Type:
Article
Institution/Affiliation country:
Secretaria da Saúde do Estado de São Paulo/BR
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