Sar studies of fluorine-substituted benzylamines and substituted 2-phenylethylamines as substrates and inactivators of monoamine oxidase b

Richard B. Silverman*, William P. Hawe

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

13 Scopus citations

Abstract

To test whether addition of electron-withdrawing substituents to good substrates of monoamine oxi-dase (MAO) will transform them into inactivators, a series of fluorine-substituted benzylamines and a series of substituted 2-phenylethylamines were synthesized and tested as substrates and inactivators of monoamine oxidase B. All of the compounds were substrates. None of the benzylamines was an inactivator, but several of the phenethylamines were. These results suggest that either stronger electron withdrawing character or additional stabilizing factors are needed to stabilize the hypothesized enzyme adduct.

Original languageEnglish (US)
Pages (from-to)203-215
Number of pages13
JournalJournal of Enzyme Inhibition and Medicinal Chemistry
Volume9
Issue number3
DOIs
StatePublished - 1995

Keywords

  • Fluorinated benzylamines
  • Monoamine oxidase B
  • Structure-activity relationships
  • Substituted 2-phenylethylamines

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery

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