Actelion Pharmaceuticals Ltd, Drug Discovery Chemistry and Biology, Hegenheimermattweg 91, CH-4123 Allschwil/BL, Switzerland.
Bioorg Med Chem Lett. 2013 Feb 1;23(3):658-62. doi: 10.1016/j.bmcl.2012.11.118. Epub 2012 Dec 11.
A novel series of anti-malarials, based on a hydroxy-ethyl-amine scaffold, initially identified as peptidomimetic protease inhibitors is described. Combination of the hydroxy-ethyl-amine anti-malarial phramacophore with the known Mannich base pharmacophore of amodiaquine (57) resulted in promising in vivo active novel derivatives.
描述了一系列新型抗疟药物，它们基于羟乙基胺支架，最初被鉴定为拟肽蛋白酶抑制剂。将羟乙基胺抗疟药效团与已知的氨喹（57）的曼尼希碱药效团组合，得到了具有前景的新型体内活性衍生物。
