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Synthesis and biological evaluation of phloroglucinol derivatives possessing α-glycosidase, acetylcholinesterase, butyrylcholinesterase, carbonic anhydrase inhibitory activity

ArticleAçık Erişim

Özet

A series of novel phloroglucinol derivatives were designed, synthesized, characterized spectroscopically and tested for their inhibitory activity against selected metabolic enzymes, including α-glycosidase, acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and human carbonic anhydrase I and II (hCA I and II). These compounds displayed nanomolar inhibition levels and showed Ki values of 1.14–3.92 nM against AChE, 0.24–1.64 nM against BChE, 6.73–51.10 nM against α-glycosidase, 1.80–5.10 nM against hCA I, and 1.14–5.45 nM against hCA II. © 2018 Deutsche Pharmazeutische Gesellschaft

Anahtar Kelimeler

acetylcholinesterasebutyrylcholinesterasecarbonic anhydrasephloroglucinol derivativesα-glycosidaseAnimalsCarbonic AnhydrasesDose-Response Relationship, DrugElectrophorusEnzyme InhibitorsGlycoside HydrolasesHorsesHumansMolecular Docking SimulationMolecular StructurePhloroglucinolStructure-Activity Relationship4 bromocinnamic acid4 bromocinnamic acid methyl ester4 bromocinnamyl alcohol4 bromocinnamyl bromide4 bromocinnamyl phloroglucinol4 chlorocinnamic acid methyl ester4 chlorocinnamyl alcohol4 chlorocinnamyl bromide4 chlorocinnamyl phloroglucinol4 fluorocinnamic acid4 fluorocinnamic acid methyl ester4 fluorocinnamyl alcohol4 fluorocinnamyl bromide
RDL Kalıcı Bağlantı (PID)
https://rdlopen.rawdatalibrary.net/r/ebyu/14268Resmi atıflarda kullanılan kalıcı adres
DOI
https://doi.org/10.1002/ardp.201700314Yayıncı resmi DOI adresi
Tam Kayıt
AlanDeğerDil
dc.contributor.authorBurmaoglu, Serdar
dc.contributor.authorYilmaz, Ali O.
dc.contributor.authorTaslimi, Parham
dc.contributor.authorAlgul, Oztekin
dc.contributor.authorKilic, Deryanur
dc.contributor.authorGulcin, Ilhami
dc.date.accessioned2026-10-18T20:29:03.620577023Z
dc.date.available2026-10-18T20:29:03.620577023Z
dc.date.issued2018
dc.description.abstractA series of novel phloroglucinol derivatives were designed, synthesized, characterized spectroscopically and tested for their inhibitory activity against selected metabolic enzymes, including α-glycosidase, acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and human carbonic anhydrase I and II (hCA I and II). These compounds displayed nanomolar inhibition levels and showed Ki values of 1.14–3.92 nM against AChE, 0.24–1.64 nM against BChE, 6.73–51.10 nM against α-glycosidase, 1.80–5.10 nM against hCA I, and 1.14–5.45 nM against hCA II. © 2018 Deutsche Pharmazeutische Gesellschaft
dc.description.sponsorshipFunding text 1: (TUBITAK, Grant Number: 114Z554) for their financial support.; Funding text 2: We thank the Scientific and Technological Research Council of Turkey
dc.identifier.doi10.1002/ardp.201700314
dc.identifier.eissn1521-4184
dc.identifier.issn0365-6233
dc.identifier.issue2
dc.identifier.pmid29323749
dc.identifier.scopus2-s2.0-85040630444
dc.identifier.startpage1700314
dc.identifier.urihttps://rdlopen.rawdatalibrary.net/r/ebyu/14268
dc.identifier.volume351
dc.identifier.wosWOS:000423801700007
dc.language.isoen
dc.publisherWiley-VCH Verlag
dc.relation.ispartofArchiv der Pharmazie
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subjectacetylcholinesterase
dc.subjectbutyrylcholinesterase
dc.subjectcarbonic anhydrase
dc.subjectphloroglucinol derivatives
dc.subjectα-glycosidase
dc.subjectAnimals
dc.subjectCarbonic Anhydrases
dc.subjectDose-Response Relationship, Drug
dc.subjectElectrophorus
dc.subjectEnzyme Inhibitors
dc.subjectGlycoside Hydrolases
dc.subjectHorses
dc.subjectHumans
dc.subjectMolecular Docking Simulation
dc.subjectMolecular Structure
dc.subjectPhloroglucinol
dc.subjectStructure-Activity Relationship
dc.subject4 bromocinnamic acid
dc.subject4 bromocinnamic acid methyl ester
dc.subject4 bromocinnamyl alcohol
dc.subject4 bromocinnamyl bromide
dc.subject4 bromocinnamyl phloroglucinol
dc.subject4 chlorocinnamic acid methyl ester
dc.subject4 chlorocinnamyl alcohol
dc.subject4 chlorocinnamyl bromide
dc.subject4 chlorocinnamyl phloroglucinol
dc.subject4 fluorocinnamic acid
dc.subject4 fluorocinnamic acid methyl ester
dc.subject4 fluorocinnamyl alcohol
dc.subject4 fluorocinnamyl bromide
dc.titleSynthesis and biological evaluation of phloroglucinol derivatives possessing α-glycosidase, acetylcholinesterase, butyrylcholinesterase, carbonic anhydrase inhibitory activity
dc.typeArticle
dspace.entity.typePublication
rdl.citation.scopus87
rdl.citation.wos85
rdl.departmentTercan Vocational High School, Erzincan University, Erzincan, Turkey.
rdl.source.indexSCOPUS
rdl.source.indexWOS
rdl.source.indexPUBMED
rdl.wos.indexScience Citation Index Expanded (SCI-EXPANDED)
rdl.wos.indexIndex Chemicus (IC)
rdl.wos.indexCurrent Chemical Reactions (CCR-EXPANDED)