1369956-97-7Relevant academic research and scientific papers
Synthesis of 2-amino-3-arylpropan-1-ols and 1-(2,3-diaminopropyl)-1,2,3- triazoles and evaluation of their antimalarial activity
D'Hooghe, Matthias,Vandekerckhove, Stephanie,Mollet, Karen,Vervisch, Karel,Dekeukeleire, Stijn,Lehoucq, Liesbeth,Lategan, Carmen,Smith, Peter J.,Chibale, Kelly,De Kimpe, Norbert
, p. 1745 - 1752 (2012/02/16)
A variety of 2-amino-3-arylpropan-1-ols, anti-2-amino-3-aryl-3- methoxypropan-1-ols and anti-2-amino-1-arylpropan-1,3-diols were prepared selectively through elaboration of trans-4-aryl-3-chloro-β-lactams. In addition, a number of 2-(azidomethyl)-aziridines was converted into novel 2-[(1,2,3-triazol-1-yl)methyl]aziridines by Cu(I)-catalyzed azide-alkyne cycloaddition, followed by microwave-assisted, regioselective ring opening by dialkylamine towards 1-(2,3-diaminopropyl)-1,2,3-triazoles. Although most of these compounds exhibited weak antiplasmodial activity, six representatives showed moderate antiplasmodial activity against both a chloroquine-sensitive and a chloroquine-resistant strain of Plasmodium falciparum with IC 50-values of 25 μM.
