Dehydrodieugenol B derivatives as antiparasitic agents: Synthesis and biological activity against Trypanosoma cruzi
Ferreira, Daiane D; Sousa, Fernanda S; Costa-Silva, Thais A; Reimão, Juliana Q; Torrecilhas, Ana C; Johns, Deidre M; Honorio, Kathia M; Lago, João Henrique G; Anderson, Edward A; Tempone, Andre G.
European Journal of Medicinal Chemistry
; 1762019.
Artículo
en Portugués
| LILACS, SES-SP, SES SP - Instituto Adolfo Lutz, SES-SP, SESSP-IALACERVO | ID: biblio-1007421
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
Biblioteca responsable:
BR91.2
Ubicación: BR76.1; P
Texto completo
Documentos relacionados