Synthesis and antiinflammation activity of aromatic aminoketone compounds, a new type of PAF-receptor antagonist

A series of aromatic aminoketones were synthesized by Mannich reaction. Structures of these compounds were confirmed by ¹H NMR, MS and HRMS or element analysis. Pharmacological screening showed that most target compounds inhibited the release of β-glucuronidase in polymorphonuclear leucocytes by PAF (platelet activating factor) and compounds MA12, MA13, MA18, MA21 and MA33 were more active. The study suggests that target compounds are potential PAF receptor antagonists and their anti-inflammatory activities are due to the inhibition of release of lysosomal enzyme.