Design, synthesis and in vitro antimalarial evaluation of triazole-linked chalcone and dienone hybrid compounds

作者：Guantai Eric M; Ncokazi Kanyile; Egan Timothy J; Gut Jiri; Rosenthal Philip J; Smith Peter J; Chibale Kelly^*

来源：Bioorganic & Medicinal Chemistry, 2010, 18(23): 8243-8256.

DOI：10.1016/j.bmc.2010.10.009

• Malaria
• Chalcones
• Dienones
• Triazole
• Hybrid compounds
• Plasmodium falciparum
• Aminoquinolines
• Nucleosides

A targeted series of chalcone and dienone hybrid compounds containing aminoquinoline and nucleoside templates was synthesized and evaluated for in vitro antimalarial activity. The Cu(I)-catalyzed cycloaddition of azides and terminal alkynes was applied as the hybridization strategy. Several chalcone-chloroquinoline hybrid compounds were found to be notably active, with compound 8b the most active, exhibiting submicromolar IC(50) values against the D10, Dd2 and W2 strains of Plasmodium falciparum.

• 出版日期2010-12-1