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Coumarin-Rasagiline Hybrids as Potent and Selective hMAO-B Inhibitors, Antioxidants, and Neuroprotective Agents

dc.contributor.authorMatos M.J.
dc.contributor.authorHerrera Ibatá D.M.
dc.contributor.authorUriarte E.
dc.contributor.authorViña D.
dc.date.accessioned2020-09-02T22:23:01Z
dc.date.available2020-09-02T22:23:01Z
dc.date.issued2020
dc.identifier10.1002/cmdc.202000018
dc.identifier.citation15, 6, 532-538
dc.identifier.issn18607179
dc.identifier.urihttps://hdl.handle.net/20.500.12728/5337
dc.descriptionThe frequency, complexity and morbidity of neurodegenerative diseases make them a great challenge for nowadays medicine. Most of the treatments currently used for Parkinson's disease – the second most prevalent – are only symptomatic. Therefore, it is urgent to develop drugs that are able to act simultaneously on different targets, being able to stop neuronal death and promote the recovery of neuronal populations already affected. In this work, we studied the activity of a series of hybrid molecules, which combine the structure of both coumarin and an alkynylamine group inspired on rasagiline, as MAO inhibitors, antioxidants and neuroprotective agents. Half of the studied hybrids turned out to be selective monoamine oxidase B (hMAO-B) inhibitors in the low micro/nanomolar range, demonstrating that positions 3 (compounds 1–3) and 7 (compounds 8 and 10) of the coumarin scaffold are the most suitable for the incorporation of the alkynylamine chain. All the studied compounds proved to be capable of neutralizing free radicals (DPPH). Finally, the 4-(but-2-yn-1-ylamino)coumarin (5) showed neuroprotective effects on glial cells and the 4-methyl-7-(pent-2-yn-1-ylamino)coumarin (8) inhibited intraneuronal ROS production as well. © 2020 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim
dc.language.isoen
dc.publisherJohn Wiley and Sons Ltd
dc.subjectAntioxidants
dc.subjectCoumarin-rasagiline hybrids
dc.subjecthMAO-B inhibitors
dc.subjectNeuroprotectors
dc.subjectParkinson's disease
dc.subject4 (but 2 yn 1 ylamino)coumarin
dc.subjectamine oxidase (flavin containing) isoenzyme B
dc.subjectantioxidant
dc.subjectcoumarin
dc.subjectmonoamine oxidase inhibitor
dc.subjectneuroprotective agent
dc.subjectrasagiline
dc.subjectunclassified drug
dc.subjectanimal experiment
dc.subjectantioxidant activity
dc.subjectArticle
dc.subjectDPPH radical scavenging assay
dc.subjectembryo
dc.subjectenzyme inhibition
dc.subjectneuroprotection
dc.subjectnonhuman
dc.subjectpriority journal
dc.subjectrat
dc.titleCoumarin-Rasagiline Hybrids as Potent and Selective hMAO-B Inhibitors, Antioxidants, and Neuroprotective Agents
dc.typeArticle


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