Transformation of monoamine oxidase-B primary amine substrates into time-dependent inhibitors. Tertiary amine homologs of primary amine substrates

…, X Lu, K Nishimura, RB Silverman

Index: Ding, Charles Z.; Lu, Xingliang; Nishimura, Kuniko; Silverman, Richard B. Journal of Medicinal Chemistry, 1993 , vol. 36, # 12 p. 1711 - 1715

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Citation Number: 16

Abstract

A family of N-methylated and N, N-dimethylated alkyl and arylalkylamines was prepared and more than half of the analogues were shown to be time-dependent pseudo-first-order inhibitors of monoamine oxidase-B. Some of the time-dependent inactivators were reversible and others were irreversible with respect to prolonged dialysis following inactivation. Partition ratios ranged from zero to 11 000. These results are rationalized in ...