Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, Via Mangiagalli 25, 20133 Milan, Italy.
Bioorg Med Chem Lett. 2012 Sep 15;22(18):5915-8. doi: 10.1016/j.bmcl.2012.07.069. Epub 2012 Jul 27.
We report the discovery of new potent inhibitors of the growth of Plasmodium falciparum chloroquine (CQ)-resistant W2 strain. These compounds were designed using the double drug approach by introducing a residue able to enhance the accumulation of plasmepsins inhibitors into the food vacuole. Some of the molecules were more active than CQ against CQ-resistant strain and showed good selectivity against cathepsin D.
我们报告了新的强效抑制剂的发现 疟原虫恶性疟原虫氯喹(CQ)-耐药 W2 株的生长。这些化合物是通过引入一个残基来设计的,该残基能够增强质体蛋白酶抑制剂在食物泡中的积累,从而采用双重药物方法设计的。一些分子比 CQ 对 CQ 耐药株更有效,并对组织蛋白酶 D 表现出良好的选择性。