scholarly journals Synthesis and evaluation of small molecules bearing a benzyloxy substituent as novel and potent monoamine oxidase inhibitors

MedChemComm ◽  
2017 ◽  
Vol 8 (2) ◽  
pp. 471-478 ◽  
Author(s):  
Jin-Shuai Lan ◽  
Tong Zhang ◽  
Yun Liu ◽  
Yong Zhang ◽  
Jian-wei Hou ◽  
...  
Keyword(s):  
Monoamine Oxidase ◽  
Small Molecules ◽  
Inhibitory Activity ◽  
Monoamine Oxidase Inhibitors

A new series of small molecules bearing a benzyloxy substituent have been designed, synthesized and evaluated for hMAO inhibitory activity in vitro.

scholarly journals Monoamine Oxidase Inhibitory Activity of Biflavonoids from Branches of Garcinia gardneriana (Clusiaceae)

2017 ◽  
Vol 12 (4) ◽  
pp. 1934578X1701200 ◽  
Author(s):  
Maria Angélica Recalde-Gil ◽  
Luiz Carlos Klein-Júnior ◽  
Carolina dos Santos Passos ◽  
Juliana Salton ◽  
Sérgio Augusto de Loreto Bordignon ◽  
...  
Keyword(s):  
Monoamine Oxidase ◽  
Inhibitory Activity ◽  
Ethanol Extract ◽  
Ethyl Acetate Fraction ◽  
Spectrometric Data ◽  
Mao B ◽  
Inhibitory Compounds ◽  
Mao A ◽  
Mao Activity

Garcinia gardneriana is chemically characterized by the presence of biflavonoids. Taking into account that flavonoids are able to inhibit monoamine oxidase (MAO) activity, in the present study, the chemical composition of the branches’ extract of the plant is described for the first time and the MAO inhibitory activity of the isolated biflavonoids was evaluated. Based on spectroscopic and spectrometric data, it was possible to identify volkesiflavone, morelloflavone (1), Gb-2a (2) and Gb-2a-7- O-glucoside (3) in the ethyl acetate fraction from ethanol extract of the branches. Compounds 1-3 were evaluated in vitro and demonstrated the capacity to inhibit MAO-A activity with an IC50 ranging from 5.05 to 10.7 μM, and from 20.7 to 66.2 μM for MAO-B. These inhibitions corroborate with previous IC50 obtained for monomeric flavonoids, with a higher selectivity for MAO-A isoform. The obtained results indicate that biflavonoids might be promising structures for the identification of new MAO inhibitory compounds.

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.

In vitro and in silico evaluation of new thiazole compounds as monoamine oxidase inhibitors

2019 ◽  
Vol 85 ◽  
pp. 97-108 ◽  
Author(s):  
Begüm Nurpelin Sağlık ◽  
Betül Kaya Çavuşoğlu ◽  
Derya Osmaniye ◽  
Serkan Levent ◽  
Ulviye Acar Çevik ◽  
...  
Keyword(s):  
Monoamine Oxidase ◽  
In Silico ◽  
Monoamine Oxidase Inhibitors

scholarly journals In Vitro and In Silico ADME-Tox Profiling and Safety Significance of Multifunctional Monoamine Oxidase Inhibitors Targeting Neurodegenerative Diseases

2020 ◽  
Vol 11 (22) ◽  
pp. 3793-3801
Author(s):  
Anna Więckowska ◽  
Natalia Szałaj ◽  
Izabella Góral ◽  
Adam Bucki ◽  
Gniewomir Latacz ◽  
...  
Keyword(s):  
Monoamine Oxidase ◽  
Neurodegenerative Diseases ◽  
In Silico ◽  
Monoamine Oxidase Inhibitors

Synthesis and in vitro study of nitro- and methoxy-2-phenylbenzofurans as human Monoamine Oxidase inhibitors

2021 ◽  
pp. 104616
Author(s):  
Giovanna L. Delogu ◽  
Amit Kumar ◽  
Gianluca Gatto ◽  
Fernando Bustelo ◽  
Lucía M. Saavedra ◽  
...  
Keyword(s):  
Monoamine Oxidase ◽  
In Vitro Study ◽  
Monoamine Oxidase Inhibitors ◽  
Vitro Study

Flavonoids and Anthranquinones as Xanthine Oxidase and Monoamine Oxidase Inhibitors: A New Approach Towards Inflammation and Oxidative Stress

2019 ◽  
Vol 18 (25) ◽  
pp. 2154-2164 ◽  
Author(s):  
Neelam Malik ◽  
Priyanka Dhiman ◽  
Eduardo Sobarzo-Sanchez ◽  
Anurag Khatkar
Keyword(s):  
Monoamine Oxidase ◽  
Xanthine Oxidase ◽  
Monoamine Oxidase Inhibitors ◽  
New Approach ◽  
Drug Substances ◽  
Structure Activity ◽  
Synthetic Drug ◽  
And Oxidative Stress ◽  
Natural And Synthetic

The development of xanthine oxidase and monoamine oxidase inhibitors led to important breakthroughs in the therapy of oxidative damage, hyperuricemia, gout, neurological, neuropsychiatric disorders and management of reperfusion injury. Drugs obtained from natural sources play an important role in the treatment of various pathological disorders and act as a lead compound for the discovery of new synthetic drug substances. In this review, various pharmacological effects produced by the inhibition of xanthine oxidase and monoamine oxidase through natural and synthetic flavonoids as well as anthraquinones are discussed in detail. Several methods have been designed for monitoring enzymatic activity and its inhibitor screening of bioactive natural and synthetic flavonoids and anthraquinones. In this review, all the in-vitro and other computational approaches are critically discussed which provided the clue about structure activity requirements for further precise modifications on the basic scaffold.

scholarly journals MAO inhibitory activity of bromo-2-phenylbenzofurans: synthesis, in vitro study, and docking calculations

MedChemComm ◽  
2017 ◽  
Vol 8 (9) ◽  
pp. 1788-1796 ◽  
Author(s):  
G. L. Delogu ◽  
F. Pintus ◽  
L. Mayán ◽  
M. J. Matos ◽  
S. Vilar ◽  
...  
Keyword(s):  
Monoamine Oxidase ◽  
Brain Development ◽  
Inhibitory Activity ◽  
In Vitro Study ◽  
Vitro Study ◽  
Monoamine Neurotransmitters ◽  
Docking Calculations ◽  
And Function

Monoamine oxidase (MAO) is an enzyme responsible for metabolism of monoamine neurotransmitters which play an important role in brain development and function.

Commonly Used Medications that Interfere with Routine Endocrine Laboratory Procedures

1964 ◽  
Vol 10 (1) ◽  
pp. 41-52 ◽  
Author(s):  
Samuel Borushek ◽  
Jay J Gold
Keyword(s):  
Monoamine Oxidase ◽  
Optical Density ◽  
Laboratory Tests ◽  
Density Measurement ◽  
Monoamine Oxidase Inhibitors ◽  
Color Development ◽  
Optical Density Measurement ◽  
Laboratory Procedures

Abstract Ten groups of commonly utilized medications were examined both in vitro and in vivo for their ability to interfere with optical density measurement and/or color development in such routine endocrine laboratory tests as those for 17-ketosteroids and 17-hydroxycorticosteroids. Certain antihypertensives, tranquilizers, psychic energizers, monoamine oxidase inhibitors, and soporifics were found to create the most problems in interference. The importance of removing these medications from the patients' therapeutic regimes prior to obtaining specimens for such endocrine procedures is stressed.

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