Chromone 3-phenylcarboxamides as potent and selective MAO-B inhibitors

Gaspar, Alexandra; Reis, Joana; Fonseca, André; Milhazes, Nuno; Viña, Dolores; Uriarte, Eugenio; Borges, Fernanda

doi:10.1016/j.bmcl.2010.11.128

Cited by 77 publications

(52 citation statements)

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“…Potential tight-binding of inhibitors to the MAOs has been previously reported for a variety of different classes of compounds. [44][45][46][47] Since the inhibition of MAO-B by compound 4h may not to be readily reversible and 4h therefore may exhibit a degree of tight-binding to the MAO-B active site, the reversibility of MAO-B inhibition by 4h was further examined by dialysis. For this purpose MAO-B and 4h, at a concentration of 4 Â IC 50 , were preincubated for a period of 15 min and subsequently dialysed for 24 h. The residual enzyme activity was measured and compared to similar dialysis experiments performed in the absence of inhibitor and presence of the irreversible inhibitor, (R)-deprenyl.…”

Section: Since Reversibility Of Mao Inhibition Is Frequently a Considmentioning

confidence: 99%

Monoamine oxidase inhibitory activities of heterocyclic chalcones

Minders

Petzer

et al. 2015

Bioorganic & Medicinal Chemistry Letters

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Section: Since Reversibility Of Mao Inhibition Is Frequently a Considmentioning

confidence: 99%

Monoamine oxidase inhibitory activities of heterocyclic chalcones

Minders

Petzer

et al. 2015

Bioorganic & Medicinal Chemistry Letters

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“…Privileged structures, such as indoles, arylpiperazines, biphenyls and benzopyranes are currently ascribed as helpful approaches. In fact, different families of nitrogen and oxygen heterocycles, such as pyrazoles, hydrazinylthiazoles, xanthones, coumarins or chromones have been extensively used as scaffolds in medicinal chemistry programs for the search of novel MAO-B inhibitors [51][52][53][54][55][56][57]. There are a large number of studies on the identification of novel potent and selective MAO inhibitors that could serve as potential lead molecules for drug discovery.…”

Section: Drug Discovery and Development Of Mao-b Inhibitorsmentioning

confidence: 99%

Parkinson's Disease Management. Part II- Discovery of MAO-B Inhibitors Based on Nitrogen Heterocycles and Analogues

Reis¹,

Encarnacao²,

Gaspar³

et al. 2012

Current Topics in Medicinal Chemistry

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Parkinson's disease (PD) is a neurodegenerative disorder mainly characterized by a progressive neurodegeneration of the dopaminergic neurons. The available pharmacological therapy for PD aims to stop the progress of symptoms, reduce disability, slowing the neurodegenerative process and/or preventing long-term complications along the therapy. The main strategic developments that have led to progress in the medical management of PD have focused on improvements in dopaminergic therapies. Despite all the recent research, there are only a few classes of drugs approved for the treatment of motor related symptoms of PD which primarily act on the dopaminergic neurons system: L-dopa, dopamine agonists, monoamine oxidase-B (MAO-B) and catechol-O-methyl transferase (COMT) inhibitors. Anticholinergic drugs and glutamate antagonists are also available but are not commonly used in routine practice. As no effective therapeutic strategy has yet been attended, other solutions must be investigated. Privileged structures, such as indoles, arylpiperazines, biphenyls and benzopyranes are currently ascribed as helpful approaches. Different families of nitrogen and oxygen heterocycles, such as pyrazoles, hydrazinylthiazoles, xanthones, coumarins or chromones have also been extensively used as scaffolds in medicinal chemistry programs for searching novel MAO-B inhibitors. Nitrogen derivatives play a key role in this subject with several studies pointing out hydrazines, thiazoles or indoles as important scaffolds for the development of novel MAO-B inhibitors. This review comprises an overview of the state of the art on the actual pharmacological therapy for PD followed by a specific focus on the discovery and development of nitrogen-based heterocyclic compounds analogues as promising MAO-B inhibitors.

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“…1), another example of a natural chromene derivative, is known for its therapeutic properties for many diseases including cancer (Singh et al, 2011). Naturally occurring chromenes are now used as valuable leads for the design and synthesis of new active analogs and synthetic derivatives incorporating the chromene scaffold, where they are reported, for example, as anti-HIV agents, monoamine oxidase and interleukin-5 inhibitors, anti-inflammatory and antibacterial agents, as well as as anticancer drugs (Vasselin et al, 2006;Chimenti et al, 2009;Nam et al, 2010;Zhou et al, 2010;Gaspar et al, 2011;Kostova et al, 2011).…”

Section: Introductionmentioning

confidence: 99%