Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
Bioorg Med Chem Lett. 2012 Aug 1;22(15):5046-50. doi: 10.1016/j.bmcl.2012.06.010. Epub 2012 Jun 9.
The synthesis and evaluation of antiplasmodial activity of benzothiazole, benzimidazole, benzoxazole and pyridine analogues of amodiaquine is hereby reported. Benzothiazole and benzoxazole analogues with a protonatable tertiary nitrogen atom possessed excellent activity against the W2 and K1 chloroquine resistant strains of Plasmodium falciparum, with IC(50)s ranging from 7 to 22 nM.
本文报道了抗疟药阿莫地喹的苯并噻唑、苯并咪唑、苯并恶唑和吡啶类似物的合成与活性评价。带有可质子化的叔氮原子的苯并噻唑和苯并恶唑类似物对疟原虫 W2 和 K1 氯喹耐药株表现出优异的活性，IC（50）范围为 7 至 22 nM。
