Synthesis of new pyrazolone-based heterocycles as inhibitors of monoamine oxidase enzymes

  • Taha M. A. Eldebss
  • Xue-Jing Yi
  • Ahmad M. Farag
  • Ahmad A. Khedr
  • Mohamed M. Abdulla
  • Yahia N. Mabkhot
Original Paper


A series of new substituted pyrazoles embedded with a variety of function groups has been synthesized from 4-[4-(1,2-dihydro-2,3-dimethyl-1-phenyl-5-oxo-3H-pyrazol-4-yl)]-2-cyano-4-oxo-butanenitrile (4). The synthesized compounds were fully characterized and their structures were elucidated based on elemental analysis, spectral data, and alternative synthetic pathways, whenever possible. The pharmacological activities of these new compounds as inhibitors for of type A and type B monoamine oxidase (MAO) enzymes have been investigated and compared to the most common inhibitors of MAO enzymes used to treat depression and anxiety such as deprenyl (selegiline), moclobemide, and clorgyline drugs. The most potent of the synthesized compounds was 4, 11, and 53 which showed higher inhibition activity toward type A MAO enzyme and even exceeded that of deprenyl, moclobemide, and clorgyline drugs.


Monoamine oxidase (MAO) enzyme Pyrazoles Type A and type B monoamine oxidase inhibitors IC50 Deprenyl 



The authors would like to extend their sincere appreciation to the Deanship of the Scientific Research at King Saud University for the support of the Research (PRG-1437-29).


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Copyright information

© Iranian Chemical Society 2018

Authors and Affiliations

  1. 1.Department of Chemistry, Faculty of ScienceCairo UniversityGizaEgypt
  2. 2.Yueyang Vocational Technical CollegeYueyangChina
  3. 3.Research UnitSaco Pharm. Co.6th October CityEgypt
  4. 4.Department of Chemistry, College of ScienceKing Saud UniversityRiyadhSaudi Arabia

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