Department of Chemistry, University of Cape Town, South Africa.
Bioorg Med Chem. 2010 Dec 1;18(23):8243-56. doi: 10.1016/j.bmc.2010.10.009. Epub 2010 Oct 31.
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.
设计并合成了一系列以氨基喹啉和核苷为模板的查尔酮和二烯酮杂合化合物，并评估了它们的体外抗疟活性。该杂化策略采用了叠氮化物和末端炔烃的 Cu(I)催化环加成反应。发现几种查尔酮-氯喹啉杂合化合物具有显著的活性，其中化合物 8b 活性最高，对恶性疟原虫 D10、Dd2 和 W2 株的 IC(50)值均低于亚微摩尔。
