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Design, synthesis and biological evaluation of novel benzocoumarin derivatives as potent inhibitors of MAO-B activity

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dc.contributor.authorMELETLİ, FURKAN
dc.contributor.authorDEMİR, SERAP
dc.contributor.authorDANIŞ, ÖZKAN
dc.contributor.authorsMELETLİ F., Gündüz C., Alparslan M. M., ATTAR A., DEMİR S., İskit E., DANIŞ Ö.
dc.date.accessioned2024-10-14T17:17:27Z
dc.date.available2024-10-14T17:17:27Z
dc.date.issued2024-11-15
dc.description.abstractThe continued research of novel reversible inhibitors targeting monoamine oxidase (MAO) B remains crucial for effectively symptomatic treatment of Parkinson\"s disease. In this study we synthesized and evaluated a new series of 3-aryl benzo[g] and benzo[h] coumarin derivatives as MAO-B inhibitors. Compound A6 has been found to display the most potent inhibitory activity and selectivity against the MAO-B isoform (IC50 = 13 nM and SI = >7693.31 respectively). Inhibition mode of A6 on MAO-B was predicted as mixed reversible inhibition with a Ki value of 3.274 nM. Furthermore, in order to elaborate structure–activity relationships, the binding mode of A6 was investigated by molecular docking simulations.
dc.identifier.citationMELETLİ F., Gündüz C., Alparslan M. M., ATTAR A., DEMİR S., İskit E., DANIŞ Ö., "Design, synthesis and biological evaluation of novel benzocoumarin derivatives as potent inhibitors of MAO-B activity", Bioorganic and Medicinal Chemistry Letters, cilt.113, 2024
dc.identifier.doi10.1016/j.bmcl.2024.129984
dc.identifier.issn0960-894X
dc.identifier.urihttps://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85205697263&origin=inward
dc.identifier.urihttps://hdl.handle.net/11424/298066
dc.identifier.volume113
dc.language.isoeng
dc.relation.ispartofBioorganic and Medicinal Chemistry Letters
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subjectTıp
dc.subjectYaşam Bilimleri
dc.subjectBiyoteknoloji
dc.subjectMoleküler Biyoloji ve Genetik
dc.subjectSitogenetik
dc.subjectKimya
dc.subjectBiyokimya
dc.subjectBiyoinorganik Kimya
dc.subjectSağlık Bilimleri
dc.subjectTemel Bilimler
dc.subjectMedicine
dc.subjectLife Sciences
dc.subjectBiotechnology
dc.subjectMolecular Biology and Genetics
dc.subjectCytogenetic
dc.subjectChemistry
dc.subjectBiochemistry
dc.subjectBioinorganic Chemistry
dc.subjectHealth Sciences
dc.subjectNatural Sciences
dc.subjectKlinik Tıp (Med)
dc.subjectTemel Bilimler (Sci)
dc.subjectYaşam Bilimleri (Life)
dc.subjectKlinik Tıp
dc.subjectMoleküler Biyoloji Ve Genetik
dc.subjectMikrobiyoloji
dc.subjectTropikal Tıp
dc.subjectKimya Organik
dc.subjectBiyokimya Ve Moleküler Biyoloji
dc.subjectBiyoteknoloji Ve Uygulamalı Mikrobiyoloji
dc.subjectClinical Medicine (Med)
dc.subjectNatural Sciences (Sci)
dc.subjectLife Sciences (Life)
dc.subjectClinical Medicine
dc.subjectMolecular Biology & Genetics
dc.subjectMicrobiology
dc.subjectTropical Medicine
dc.subjectChemistry Organic
dc.subjectBiochemistry & Molecular Biology
dc.subjectBiotechnology & Applied Microbiology
dc.subjectMoleküler Tıp
dc.subjectMoleküler Biyoloji
dc.subjectFarmasötik bilim
dc.subjectİlaç Keşfi
dc.subjectKlinik Biyokimya
dc.subjectOrganik Kimya
dc.subjectFizik Bilimleri
dc.subjectMolecular Medicine
dc.subjectMolecular Biology
dc.subjectPharmaceutical Science
dc.subjectDrug Discovery
dc.subjectClinical Biochemistry
dc.subjectOrganic Chemistry
dc.subjectPhysical Sciences
dc.subjectBenzo[g]coumarin
dc.subjectBenzo[h]coumarin
dc.subjectMolecular docking
dc.subjectMonoamine oxidase
dc.subjectParkinson's Disease
dc.titleDesign, synthesis and biological evaluation of novel benzocoumarin derivatives as potent inhibitors of MAO-B activity
dc.typearticle
dspace.entity.typePublication
local.avesis.idf1ca3247-903a-4fea-b227-cabaf40e1e4b
local.indexed.atSCOPUS
relation.isAuthorOfPublicatione691a304-c784-411a-9349-f69fc9e9682a
relation.isAuthorOfPublication2790d85f-c14d-4e37-8567-e89f9e168058
relation.isAuthorOfPublication91b82a1e-bb32-4e40-ad53-90dcac92bacd
relation.isAuthorOfPublication.latestForDiscoverye691a304-c784-411a-9349-f69fc9e9682a

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