Synthesis and evaluation of new antimalarial phenylurenyl chalcone derivatives

摘要

Phenylurenyl chalcone derivatives have been synthesized and tested as inhibitors of in vitro development of a chloroquine-resistant strain of Plasmodium falciparum, activity of the cysteme protease falcipain-2, in vitro globin hydrolysis, β-hematin formation, and murine Plasmodium berghei malaria. The most active antimalarial compound was 1-[3'-N'-(N'-phenylurenyl)phenyl]-3(3,4,5-trimethoxyphenyl)-2-propen-1-one 49, with an IC50 of 1.76 μ M for inhibition of P. falciparum development. Results suggest that chalcones exert their antimalarial activity via multiple mechanisms.