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