In this work six diversely substituted N-propargylated-1,3,5-triazines have been designed, synthesized, and evaluated as monoamine oxidase (MAO) inhibitors. Very surprisingly, only 4,6-dichloro-N-(prop-2-yn-1-yl)-1,3,5-triazin-2-amine (1) showed modest, but selective MAO−B inhibition (IC50=14.2 ± 0.7 μM), whose binding affinity has been investigated by computational analysis.

Synthesis, Monoamine Oxidase Inhibition and Computational Analysis of Diversely Substituted N-Propargylated-1,3,5-triazines

Alcaro S.;Ortuso F.;
2019-01-01

Abstract

In this work six diversely substituted N-propargylated-1,3,5-triazines have been designed, synthesized, and evaluated as monoamine oxidase (MAO) inhibitors. Very surprisingly, only 4,6-dichloro-N-(prop-2-yn-1-yl)-1,3,5-triazin-2-amine (1) showed modest, but selective MAO−B inhibition (IC50=14.2 ± 0.7 μM), whose binding affinity has been investigated by computational analysis.
2019
1,3,5-triazines
Computational analysis
monoamine oxidase enzyme inhibition
N-propargyl amines
synthesis
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/20.500.12317/63423
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