scholarly journals Reversible and irreversible small molecule inhibitors of monoamine oxidase B (MAO-B) investigated by biophysical techniques

2015 ◽  
Vol 23 (4) ◽  
pp. 770-778 ◽  
Author(s):  
Rafael J. Rojas ◽  
Dale E. Edmondson ◽  
Terri Almos ◽  
Roderick Scott ◽  
Mark E. Massari
Keyword(s):  
Monoamine Oxidase ◽  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Monoamine Oxidase B ◽  
Mao B ◽  
Biophysical Techniques

Acetophenone derivatives: novel and potent small molecule inhibitors of monoamine oxidase B

MedChemComm ◽  
2015 ◽  
Vol 6 (12) ◽  
pp. 2146-2157 ◽  
Author(s):  
Zhi-Min Wang ◽  
Xue-Mei Li ◽  
Wei Xu ◽  
Fan Li ◽  
Jin Wang ◽  
...  
Keyword(s):  
Monoamine Oxidase ◽  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Monoamine Oxidase B ◽  
Mao B ◽  
Acetophenone Derivatives

Compounds 1j and 2e were both potent and selective MAO-B inhibitors.

scholarly journals Correction: Acetophenone derivatives: novel and potent small molecule inhibitors of monoamine oxidase B

MedChemComm ◽  
2015 ◽  
Vol 6 (12) ◽  
pp. 2234-2234
Author(s):  
Zhi-Min Wang ◽  
Xue-Mei Li ◽  
Wei Xu ◽  
Fan Li ◽  
Jin Wang ◽  
...  
Keyword(s):  
Monoamine Oxidase ◽  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Monoamine Oxidase B ◽  
Acetophenone Derivatives

scholarly journals 4-Phenethyl-1-Propargylpiperidine-Derived Dual Inhibitors of Butyrylcholinesterase and Monoamine Oxidase B

Molecules ◽  
2021 ◽  
Vol 26 (14) ◽  
pp. 4118
Author(s):  
Tjaša Mazej ◽  
Damijan Knez ◽  
Anže Meden ◽  
Stanislav Gobec ◽  
Matej Sova
Keyword(s):  
Monoamine Oxidase ◽  
Docking Studies ◽  
Monoamine Oxidase B ◽  
Mao B ◽  
Initial Expectation ◽  
Excellent Starting Point ◽  
Starting Point ◽  
Dependent Inhibition ◽  
Dual Inhibitors ◽  
Time Dependent Inhibition

The multi-target-directed ligands (MTDLs) strategy is encouraged for the development of novel modulators targeting multiple pathways in the neurodegenerative cascade typical for Alzheimer’s disease (AD). Based on the structure of an in-house irreversible monoamine oxidase B (MAO-B) inhibitor, we aimed to introduce a carbamate moiety on the aromatic ring to impart cholinesterase (ChE) inhibition, and to furnish multifunctional ligands targeting two enzymes that are intricately involved in AD pathobiology. In this study, we synthesized three dual hMAO-B/hBChE inhibitors 13–15, with compound 15 exhibiting balanced, low micromolar inhibition of hMAO-B (IC50 of 4.3 µM) and hBChE (IC50 of 8.5 µM). The docking studies and time-dependent inhibition of hBChE confirmed the initial expectation that the introduced carbamate moiety is responsible for covalent inhibition. Therefore, dual-acting compound 15 represents an excellent starting point for further optimization of balanced MTDLs.

▼ Safinamide for Parkinson’s disease

2018 ◽  
Vol 56 (5) ◽  
pp. 54-57
Keyword(s):  
Parkinson’S Disease ◽  
Parkinson's Disease ◽  
Monoamine Oxidase ◽  
Motor Fluctuations ◽  
Daily Activities ◽  
Monoamine Oxidase B ◽  
Motor Symptoms ◽  
Idiopathic Parkinson’S Disease ◽  
Mao B ◽  
Idiopathic Parkinson's Disease

▼ Safinamide (Xadago - Zambon S.p.A) is a monoamine-oxidase B (MAO-B) inhibitor licensed as add-on therapy for people with idiopathic Parkinson’s disease who are experiencing motor fluctuations with levodopa.1 Currently there is no cure for Parkinson’s disease and drugs are used to reduce motor symptoms and improve daily activities.2,3 Here, we review the evidence for this MAO-B inhibitor.

scholarly journals Coumarin analogue 3-methyl-7H-furo[3,2-g] chromen-7-one as a possible antiparkinsonian agent

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
Keyword(s):  
Antioxidant Activity ◽  
Monoamine Oxidase ◽  
Mouse Models ◽  
Inhibitory Activity ◽  
Ex Vivo ◽  
Monoamine Oxidase B ◽  
Mao B ◽  
Continue Research ◽  
Substituted Coumarins

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.

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