Design And Synthesis Of 3-Arylcoumerin Derivatives As A Selective Mao-B Inhibitor

Abstract

Background: According to WHO Parkinson's disease affects 1-2 people 1000 of the population. Parkinson's disease increases with age and affects 1% of the population 60 years above. Parkinson’s disease is a long-term degenerative disorder of the central nervous system that mainly affects the motor system.

Objectives: The present work aimed to design and synthesize of 3-arylcoumarin derivatives which may be of better pharmacological activity with lesser adverse effects. MAO-B inhibitors are used for the treatment of Parkinson’s disease. Due to lack of affinity and selectivity, most of the currently used MAO inhibitors, i.e., iproniazid and tranylcypromine show various side effects such as hepatotoxicity and cheese reaction. To minimize the side effect, we try to design with fewer side effects.

Methods: A novel series of 3-arylcoumarin derivatives, molecules 3-(3-(2-hydroxypropyl)phenyl)-6-methyl-2H-chromen-2-one were synthesized and evaluated for their antiparkinson activity. The structures of the compound have been confirmed by spectral analysis. The molecular docking study was performed for finding the binding affinity of the GABAA receptor to rationalize their antiparkinson activities qualitatively. A quantitative estimate of drug likeness was also performed which calculated the molecular properties and screened the molecules based on drug-likeness rules and one compound was synthesized.Results: Compounds 3-(3-(2-hydroxypropyl)phenyl)-6-methyl-2H-chromen-2-one are synthesis and characterized by  FTIR and ¹H NMR spectroscopy.