Department of Sustainable Organic Chemistry and Technology, Faculty of Bioscience Engineering, Ghent University, Coupure Links 653, B-9000 Ghent, Belgium.
Eur J Med Chem. 2011 Feb;46(2):579-87. doi: 10.1016/j.ejmech.2010.11.037. Epub 2010 Dec 1.
A variety of 2-(aminomethyl)aziridines was prepared and converted into the corresponding 1,2,3-triaminopropanes through a novel, microwave-assisted and regioselective ring opening by diethylamine in acetonitrile. Antiplasmodial assays revealed antimalarial activity for 2-[(1,2,4-triazol-1-yl)methyl]aziridines and 2-(N,N-diethylaminomethyl)aziridines, as well as for the corresponding 1-(diethylamino)propanes obtained through ring opening, pointing to the relevance of both the 2-(aminomethyl)aziridine and the 1,2,3-triaminopropane unit as novel antimalarial pharmacophores.
合成了多种 2-（氨甲基）氮丙啶，并通过在乙腈中用二乙胺进行新型、微波辅助和区域选择性开环反应，将其转化为相应的 1,2,3-三氨基丙烷。抗疟原虫试验表明，2-[(1,2,4-三唑-1-基)甲基]氮丙啶和 2-(N,N-二乙氨基甲基)氮丙啶以及通过开环得到的相应的 1-(二乙氨基)丙烷具有抗疟活性，这表明 2-(氨甲基)氮丙啶和 1,2,3-三氨基丙烷单元均为新型抗疟药效团。
