Document Report Card

ID: ALA1141931

Journal: J Med Chem

Title: Synthesis and evaluation of new antimalarial phenylurenyl chalcone derivatives.

Authors: Domínguez JN, León C, Rodrigues J, Gamboa de Domínguez N, Gut J, Rosenthal PJ.

Abstract: 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 cysteine protease falcipain-2, in vitro globin hydrolysis, beta-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 IC(50) of 1.76 microM for inhibition of P. falciparum development. Results suggest that chalcones exert their antimalarial activity via multiple mechanisms.

CiteXplore: 15887974

DOI: 10.1021/jm058208o