Synthesis and antimalarial activity of urenyl Bis-chalcone in vitro and in vivo

Abstract

Some novel derivatives of Bis-chalcone were synthesized and characterized by their physical and spectral data. All the synthesized compounds were subsequently screened for in vitro globin hydrolysis, β-hematin formation, and murine Plasmodium berghei, using chloroquine as the reference drug. Most of the synthesized compounds exhibited mild to moderate susceptibilities toward the parasite in comparison with the standard. The most active antimalarial compound was 1,1-Bis-[(3′,4′-N-(urenylphenyl)-3-(3″,4″,5″-trimethoxyphenyl)]-2-propen-1-one 5, with a percentage of inhibition of heme polymerization of 87.05 ± 0.77, and this compound increased the survival time after infection, reduce the parasitemia and delay the progression of malaria.

Keywords::

• Antimalarial
• Bis-chalcone
• Plasmodium berghei
• urenyl

Acknowledgments

The study was supported by Consejo de Desarrollo Científico y Humanístico Universidad Central de Venezuela. CDCH, Grants PI 06-7477-2009, Universidad Pedagógica Experimental Libertador, Instituto Pedagógico de Caracas. CICNAT No. 09-066.

Declaration of interest

The authors report no conflicts of interest.