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N-Alkyloxycarbonyl derivatives of ethylene diamine as monoamine oxidase inhibitors

  • V. F. Pozdnev
  • A. Z. Kirkel
  • N. S. Kamyshanskaya
  • L. N. Axenova
  • A. E. Medvedev
Part of the Journal of Neural Transmission. Supplement book series (NEURAL SUPPL, volume 52)

Summary

A series of urethane type derivatives of ethylene diamine (EDA) was synthesised and tested as inhibitors of monoamine oxidase (MAO) A and B. Nature of aromatic ring and a position of substituents in it were important for the inhibitory activity. Chlorobenzyloxycarbonyl-EDA derivatives exhibited selective inhibition of MAO-A with 3,4-Cl2-QH4CH2OCO-ED A being a most potent and selective MAO-A inhibitor (IC50 4μM). Within the compounds studied, 3,4- dichloro-benzyloxycarbonyl-EDA exhibited most potent inhibition of MAO-A. This compound inhibited the activity of rat liver MAOA non-competitively with Ki (slope) value of 3.6 μM, whereas the inhibition of rat liver MAO-B was competitive with Ki (slope) value of 56 μM (not shown). 2,4-Dichlorobenzyloxycarbonyl-EDA also inhibited rat liver MAO-A in a non-competitive manner with Ki of 14.6 μM.

Keywords

Monoamine Oxidase Biomedical Chemistry Diphenyl Carbonate Liver MAOA Trichloroacetyl Chloride 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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Copyright information

© Springer-Verlag Wien 1998

Authors and Affiliations

  • V. F. Pozdnev
    • 1
  • A. Z. Kirkel
    • 1
  • N. S. Kamyshanskaya
    • 1
  • L. N. Axenova
    • 1
  • A. E. Medvedev
    • 1
    • 1
  1. 1.Institute of Biomedical ChemistryRussian Academy of Medical SciencesMoscowRussia

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