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Time-dependent slowly-reversible inhibition of monoamine oxidase A by N-substituted 1, 2, 3, 6-tetrahydropyridines

W Wichitnithad, JP O'Callaghan, DB Miller…

文献索引:Wichitnithad, Wisut; O'Callaghan, James P.; Miller, Diane B.; Train, Brian C.; Callery, Patrick S. Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 24 p. 7482 - 7492

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被引用次数: 8

摘要

A novel class of N-substituted tetrahydropyridine derivatives was found to have multiple kinetic mechanisms of monoamine oxidase A inhibition. Eleven structurally similar tetrahydropyridine derivatives were synthesized and evaluated as inhibitors of MAO-A and MAO-B. The most potent MAO-A inhibitor in the series, 2, 4-dichlorophenoxypropyl analog 12, displayed time-dependent mixed noncompetitive inhibition. The inhibition was ...