Selective inhibitors of monoamine oxidase. 2. Arylamide SAR

M Harfenist, CT Joyner, PD Mize…

Index: Harfenist, Morton; Joyner, Charles T.; Mize, Patrick D.; White, Helen L. Journal of Medicinal Chemistry, 1994 , vol. 37, # 13 p. 2085 - 2089

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Citation Number: 36

Abstract

Monoamine oxidase (MAO) exists in two forms distinguishable by substrate specificity. Inhibition of MA 0 A is believed to be responsible for the antidepressant activity of MA0 inhibitors. A group of N-arylacetamides are highly specific inhibitors of MA0 A, some with ICs0 values in the 10-100 nM range. The requirements for high activity and specificity include a nearly linear tricyclic aromatic portion but a larger and a smaller central ring ...