New2-[(5-Methoxy-1-Methylindolyl)]-Alkylamine Derivatives: the Effect of Branching and Elongation of the Side Chain on Mao Inhibition

Abstract

A novel series of previously synthesised 2-[(5-methoxy-l-methylindolyl)]alkylamine derivatives were irreversible and time-dependent mechanism-based inhibitors of MAO. The effect of branching and elongation of the side chain was evaluated on the inhibitory potency towards MAO-A and MAO-B activities. The K₁ of the reversible step and the k_inact of the irreversible one were determined in each case. The results obtained lead to the conclusion that neither the elongation nor the branching of the side chain improve the potency of the compounds as MAO inhibitors.

Key Words:

• Monoamine oxidase
• Inhibition
• Indolalkylamine derivatives
• Kinetics