Enzyme-activated irreversible inhibitors of monoamine oxidase: phenylallylamine structure-activity relationships

…, JM Lacoste, P Bey, MG Palfreyman…

Index: McDonald; Lacoste; Bey; Palfreyman; Zreika Journal of Medicinal Chemistry, 1985 , vol. 28, # 2 p. 186 - 193

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Citation Number: 104

Abstract

Seventeen 2-aryl-3-haloallylamine derivatives were prepared and evaluated as inhibitors of monoamine oxidase (MAO, EC 1.4. 3.4). The synthesis of these compounds was achieved from either a-methylstyrene or ring-substituted phenylacetic acid derivatives. With one exception, these 2-arylallylamines were found to be enzyme-activated, irreversible inhibitors of MAO. The most potent inhibitors were ring-substituted derivatives of (E)-2-phenyl-3- ...