Design, Synthesis and Docking Calculations of Prenylated Chalcones as Selective Monoamine Oxidase B Inhibitors with Antioxidant Activity

2019 ◽  
Vol 4 (26) ◽  
pp. 7698-7703 ◽  
Author(s):  
Marco Mellado ◽  
Cristian O. Salas ◽  
Eugenio Uriarte ◽  
Dolores Viña ◽  
Carlos Jara‐Gutiérrez ◽  
...  
Biomédica ◽  
2019 ◽  
Vol 39 (3) ◽  
pp. 491-501
Author(s):  
María del Pilar Olaya ◽  
Nadezdha Esperanza Vergel ◽  
José Luis López ◽  
María Dolores Viña ◽  
Mario Francisco Guerrero

Introduction: Parkinson’s disease is the second most common neurodegenerative disease. Monoamine oxidase B inhibitors are used in the treatment of this disease concomitantly with levodopa or as monotherapy. Several substituted coumarins have shown activity as inhibitors of monoamine oxidase B.Objective: To evaluate the possible antiparkinsonian effects of the coumarin analogue FCS005 (3-methyl-7H-furo[3,2-g]chromen-7-one) in mouse models, as well as its inhibitory activity towards monoamine oxidases (MAO) and its antioxidant activity.Materials and methods: FCS005 was synthesized and the reversal of hypokinesia was evaluated in the reserpine and levodopa models. Moreover, in the haloperidol model, its anticataleptic effects were evaluated. Additionally, the monoamine oxidase inhibitory activity and antioxidant activity of FCS005 were evaluated using in vitro and ex vivo studies, respectively.Results: FCS005 (100 mg/kg) caused the reversal of hypokinesia in the reserpine and levodopa models. This furocoumarin also presented anti-cataleptic effects at the same dose. Besides, it showed selective inhibitory activity towards the MAO-B isoform and antioxidant activity.Conclusion: These results attribute interesting properties to the compound FCS005. It is important to continue research on this molecule considering that it could be a potential antiparkinsonian agent.


2000 ◽  
Vol 60 (5) ◽  
pp. 709-716 ◽  
Author(s):  
R.Preston Mason ◽  
Edwin G. Olmstead ◽  
Robert F. Jacob

2016 ◽  
Vol 24 (20) ◽  
pp. 4835-4854 ◽  
Author(s):  
Ornella Di Pietro ◽  
Nelson Alencar ◽  
Gerard Esteban ◽  
Elisabet Viayna ◽  
Natalia Szałaj ◽  
...  

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