Enzyme inhibitor
he multi-target enzyme inhibitor (FW = g/mol), also known as N-((5-(3- (1-benzylpiperidin-4-yl)propoxy)-1-methyl-1H-indol-2-yl)methyl)-N- methylprop-2-yn-1-amine, bears the MAO-inhibiting propargyl group attached to a cholinesterase-inhibiting donepezil moiety retains the ability to inhibit human acetyl- and butyryl-cholinesterases as well as monamine oxidases. With a kinact/KI value of 3 × 106 min? 1 M? 1 , ASS234 inhibition of MAO A and MAO B by ASS234 is almost as effective as clorgyline. It also forms the same N5 -adduct with the isoalloxazine ring of the FAD cofactor. The kinetic studies demonstrate that ASS234 is not only a reversible inhibitor of both acetyl and butyryl-cholinesterases with μM affinity, but is also a highly potent irreversible inhibitor of MAO A similarly to clorgyline.
