Department of Chemistry, University of Cape Town, Private Bag X3, Rondebosch 7701, South Africa.
MRC/NHLS/UCT Molecular Mycobacteriology Research Unit, Division of Medical Microbiology, Department of Clinical Laboratory Sciences, University of Cape Town, Rondebosch 7701, South Africa.
Bioorg Med Chem Lett. 2014 Jan 15;24(2):560-4. doi: 10.1016/j.bmcl.2013.12.022. Epub 2013 Dec 12.
A series of compounds derived from the 2-amino-4-(2-pyridyl) thiazole scaffold was synthesized and tested for in vitro antimycobacterial activity against the Mycobacterium tuberculosis H37Rv strain, antiplasmodial activity against the chloroquine sensitive NF54 Plasmodium falciparum strain and cytotoxicity on a mammalian cell line. Optimal antimycobacterial activity was found with compounds with a 2-pyridyl ring at position 4 of the thiazole scaffold, a substituted phenyl ring at the 2-amino position, and an amide linker between the scaffold and the substituted phenyl. The antiplasmodial activity was best with compounds that had the phenyl ring substituted with hydrophobic electron withdrawing groups.
一系列源自 2-氨基-4-(2-吡啶基)噻唑骨架的化合物被合成并测试了它们对结核分枝杆菌 H37Rv 菌株的体外抗分枝杆菌活性、对氯喹敏感的 NF54 恶性疟原虫菌株的抗疟原虫活性以及对哺乳动物细胞系的细胞毒性。具有噻唑骨架 4 位上的吡啶环、2-氨基位置上的取代苯基环以及骨架和取代苯基之间的酰胺连接基的化合物表现出最佳的抗分枝杆菌活性。具有带有疏电子吸电子基团取代的苯基环的化合物表现出最佳的抗疟原虫活性。
