New Analogues of N-(2-Aminoethyl)-4-chlorobenzamide (Ro 16-6491). Some of the Most Potent Monoamine Oxidase-B Inactivators

Nikoi Annan, Richard B Silverman*

*Corresponding author for this work

Research output: Contribution to journalComment/debate

12 Scopus citations

Abstract

A series of halo- and nitro-substituted analogues of N-(2-aminoethyl)benzamide has been synthesized. All of the compounds are competitive, time-dependent inhibitors of monoamine oxidase-B (MAO-B), but upon dialysis complete return of enzyme activity is observed for all compounds. Therefore, these are mechanism-based reversible inhibitors of MAO-B. The relative potencies of the compounds are rationalized in terms of steric and hydrophobic effects.

Original languageEnglish (US)
Pages (from-to)3968-3970
Number of pages3
JournalJournal of Medicinal Chemistry
Volume36
Issue number24
DOIs
StatePublished - Jan 1 1993

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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