scholarly journals Combined structure- and ligand-based virtual screening to evaluate caulerpin analogs with potential inhibitory activity against monoamine oxidase B

2015 ◽  
Vol 25 (6) ◽  
pp. 690-697 ◽  
Author(s):  
Vitor Prates Lorenzo ◽  
José Maria Barbosa Filho ◽  
Luciana Scotti ◽  
Marcus Tullius Scotti
Keyword(s):  
Virtual Screening ◽  
Monoamine Oxidase ◽  
Inhibitory Activity ◽  
Monoamine Oxidase B ◽  
Combined Structure

Ligand-Based Virtual Screening Using Tailored Ensembles: A Prioritization Tool for Dual A2A Adenosine Receptor Antagonists / Monoamine Oxidase B Inhibitors

2016 ◽  
Vol 22 (21) ◽  
pp. 3082-3096 ◽  
Author(s):  
Aliuska Morales Helguera ◽  
Yunierkis Perez-Castillo ◽  
M. Natália D.S. Cordeiro ◽  
Eduardo Tejera ◽  
César Paz-y-Miño ◽  
...  
Keyword(s):  
Virtual Screening ◽  
Monoamine Oxidase ◽  
Adenosine Receptor ◽  
Monoamine Oxidase B ◽  
Receptor Antagonists ◽  
A2a Adenosine Receptor

scholarly journals 8-Propyl-6H-[1,3]dioxolo[4,5-g]chromen-6-one: A new coumarin with monoamine oxidase B inhibitory activity and possible anti-parkinsonian effects

2020 ◽  
Vol 56 ◽  
Author(s):  
María del Pilar Olaya ◽  
Nadezdha Esperanza Vergel ◽  
Jose Luis López ◽  
Dolores Viña ◽  
Mario Francisco Guerrero
Keyword(s):  
Monoamine Oxidase ◽  
Inhibitory Activity ◽  
Monoamine Oxidase B

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.

Identification of novel monoamine oxidase B inhibitors by structure-based virtual screening

2010 ◽  
Vol 20 (17) ◽  
pp. 5295-5298 ◽  
Author(s):  
Werner J. Geldenhuys ◽  
Altaf S. Darvesh ◽  
Max O. Funk ◽  
Cornelis J. Van der Schyf ◽  
Richard T. Carroll
Keyword(s):  
Virtual Screening ◽  
Monoamine Oxidase ◽  
Monoamine Oxidase B

scholarly journals Virtual screening tailored ensembles of QSAR models for the discovery of dual A2A Adenosine Receptor Antagonists / Monoamine Oxidase B Inhibitors

2015 ◽  
Author(s):  
Fernanda Borges ◽  
Maykel Cruz-Monteagudo ◽  
Aliuska Morales-Helguera ◽  
Yunierkis Pérez-Castillo ◽  
M. Natália D. S. Cordeiro ◽  
...  
Keyword(s):  
Virtual Screening ◽  
Monoamine Oxidase ◽  
Adenosine Receptor ◽  
Monoamine Oxidase B ◽  
Receptor Antagonists ◽  
Qsar Models

scholarly journals Dual Target Ligands with 4-tert-Butylphenoxy Scaffold as Histamine H3 Receptor Antagonists and Monoamine Oxidase B Inhibitors

2020 ◽  
Vol 21 (10) ◽  
pp. 3411 ◽  
Author(s):  
Dorota Łażewska ◽  
Agnieszka Olejarz-Maciej ◽  
David Reiner ◽  
Maria Kaleta ◽  
Gniewomir Latacz ◽  
...  
Keyword(s):  
Monoamine Oxidase ◽  
Inhibitory Activity ◽  
In Vivo Studies ◽  
Monoamine Oxidase B ◽  
Histamine H3 Receptor ◽  
Mao B ◽  
Positive Effects ◽  
H3 Receptor ◽  
Dual Target ◽  
Histamine H3

Dual target ligands are a promising concept for the treatment of Parkinson’s disease (PD). A combination of monoamine oxidase B (MAO B) inhibition with histamine H3 receptor (H3R) antagonism could have positive effects on dopamine regulation. Thus, a series of twenty-seven 4-tert-butylphenoxyalkoxyamines were designed as potential dual-target ligands for PD based on the structure of 1-(3-(4-tert-butylphenoxy)propyl)piperidine (DL76). Probed modifications included the introduction of different cyclic amines and elongation of the alkyl chain. Synthesized compounds were investigated for human H3R (hH3R) affinity and human MAO B (hMAO B) inhibitory activity. Most compounds showed good hH3R affinities with Ki values below 400 nM, and some of them showed potent inhibitory activity for hMAO B with IC50 values below 50 nM. However, the most balanced activity against both biological targets showed DL76 (hH3R: Ki = 38 nM and hMAO B: IC50 = 48 nM). Thus, DL76 was chosen for further studies, revealing the nontoxic nature of DL76 in HEK293 and neuroblastoma SH-SY5Ycells. However, no neuroprotective effect was observed for DL76 in hydrogen peroxide-treated neuroblastoma SH-SY5Y cells. Furthermore, in vivo studies showed antiparkinsonian activity of DL76 in haloperidol-induced catalepsy (Cross Leg Position Test) at a dose of 50 mg/kg body weight.

The relationship between isatin and monoamine oxidase-B inhibitory activity in urine

1996 ◽  
Vol 12 (1) ◽  
pp. 35-42 ◽  
Author(s):  
F-Y. Pang ◽  
F.H. Hucklebridge ◽  
G. Forster ◽  
K. Tan ◽  
A. Clow
Keyword(s):  
Monoamine Oxidase ◽  
Inhibitory Activity ◽  
Monoamine Oxidase B ◽  
The Relationship
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