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Monoamine oxidase inhibitory activities of novel 3,4-dihydroquinolin-(1H)-2-one derivatives

  • Amine oxidase structure and function
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Summary

Three 3,4-dihydroquinoline-(1H)-2-one derivatives were synthesized and their monoamine oxidase (MAO) inhibitory activities were evaluated. The calculated IC50 values revealed that compound Q (N-amino-3,4-dihydroquinoline-(1H)-2-one), which carries a free amine group in the molecule, inhibited rat liver MAO-B competitively and reversibly suggesting that this relatively small compound may interact with the active site channel of the enzyme while the compounds QB (1-(benzlyden-amino)-3,4-dihydroquinoline-(1H)-2-one), PCN (2-(3-cyano-2-oxo-4-phenyl-2H-quinolin-1-yl-N-cyclohexyl-2-(4-chlorophenyl) acetamide) and MG (tert-butyl-N-[cyclohexylcarbamoyl-(3-hydroxyphenyl)methyl]-N-(2-benzoylphenyl)-carbamate) inhibited rat liver MAO-B non-competitively and irreversibly, suggesting that these compounds may interact with another hydrophobic binding region outside of the active site of the enzyme.

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Authors and Affiliations

  1. Department of Basic Pharmaceutical Sciences, Faculty of Pharmacy, Haçettepe University, Ankara, Turkey

    S. G. Sunal & A. Yesilada

  2. Department of Biochemistry, Faculty of Pharmacy, Haçettepe University, Ankara, Turkey

    S. Yabanoglu & G. Ucar

Authors
  1. S. G. Sunal
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  2. S. Yabanoglu
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  3. A. Yesilada
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  4. G. Ucar
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Sunal, S., Yabanoglu, S., Yesilada, A. et al. Monoamine oxidase inhibitory activities of novel 3,4-dihydroquinolin-(1H)-2-one derivatives. J Neural Transm 114, 717–719 (2007). https://doi.org/10.1007/s00702-007-0677-9

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  • DOI: https://doi.org/10.1007/s00702-007-0677-9

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