Synthesis and antiplasmodial activity of lycorine derivatives.

Basic Information

ID: ALA1177653

Journal: Bioorg Med Chem

Title: Synthesis and antiplasmodial activity of lycorine derivatives.

Authors: Cedrón JC, Gutiérrez D, Flores N, Ravelo AG, Estévez-Braun A.

Abstract: Twenty seven lycorine derivatives were prepared and evaluated for their in vitro antimalarial activity against chloroquine-sensitive strains of Plasmodium falciparum. The best antiplasmodial activities were achieved with lycorine derivatives that present free hydroxyl groups at C-1 and C-2 or esterified as acetates or isobutyrates. The double bond C-2-C-3 is also important for the activity. Concerning to the antiplasmodial activity of the secolycorines, the higher values were obtained with the replacement of the methylenedioxy moiety by hydroxyl or acetate groups and with methyl substituent attached to the nitrogen atom.

CiteXplore: 20627737

DOI: 10.1016/j.bmc.2010.05.023

Patent ID: