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Synthesis and carbonic anhydrase inhibitory properties of novel bromophenols including natural products

MakaleAçık ErişimScopus SJRQ2
  • SDG 3 · Sağlık ve Kaliteli Yaşam

Özet

(2-Bromo-3,4-dimethoxyphenyl) (3,4-dimethoxyphenyl)methanone (10) and its derivatives with Br, one dibromide and isomeric three tribromides, were synthesized. Demethylation of these compounds afforded a series of new bromophenols. Inhibition of human cytosolic carbonic anhydrase II (hCA II) isozyme by these new bromophenols and naturally occurring 3,4,6-tribromo-5-(2,5- dibromo-3,4-dihydroxybenzyl)benzene-1,2-diol (3), and 5,5′-methylenebis(3, 4,6-tribromo-benzene-1,2-diol) (4) was investigated. The synthesized compounds showed carbonic anhydrase inhibitory capacities with IC 50 values in the range of 0.7372 μM against hCA II. Some bromophenols investigated here showed effective hCA II inhibitory activity and might be used as leads for generating novel carbonic anhydrase inhibitors which are valuable drug candidates for the treatment of glaucoma, epilepsy, gastric and duodenal ulcers, neurological disorders, or osteoporosis.

Anahtar Kelimeler

BromophenolsCarbonic anhydraseDiphenylmethaneEnzyme inhibitionGlaucoma
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Atıflar
Scopus
42
WoS
43
OpenAlex
41
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Tam Kayıt
AlanDeğerDil
dc.contributor.authorBalaydiin, Halis Türker
dc.contributor.authorSoyut, Hakan
dc.contributor.authorEkinci, Deniz
dc.contributor.authorGöksu, Sleyman
dc.contributor.authorBeydemir, Şkrü
dc.contributor.authorMenzek, Abdullah
dc.contributor.authorŞahin, Ertan
dc.date.accessioned2026-10-29T19:11:43.325934213Z
dc.date.available2026-10-29T19:11:43.325934213Z
dc.date.issued2012
dc.description.abstract(2-Bromo-3,4-dimethoxyphenyl) (3,4-dimethoxyphenyl)methanone (10) and its derivatives with Br, one dibromide and isomeric three tribromides, were synthesized. Demethylation of these compounds afforded a series of new bromophenols. Inhibition of human cytosolic carbonic anhydrase II (hCA II) isozyme by these new bromophenols and naturally occurring 3,4,6-tribromo-5-(2,5- dibromo-3,4-dihydroxybenzyl)benzene-1,2-diol (3), and 5,5′-methylenebis(3, 4,6-tribromo-benzene-1,2-diol) (4) was investigated. The synthesized compounds showed carbonic anhydrase inhibitory capacities with IC 50 values in the range of 0.7372 μM against hCA II. Some bromophenols investigated here showed effective hCA II inhibitory activity and might be used as leads for generating novel carbonic anhydrase inhibitors which are valuable drug candidates for the treatment of glaucoma, epilepsy, gastric and duodenal ulcers, neurological disorders, or osteoporosis.
dc.description.sponsorshipTÜBİTAK
dc.description.sponsorshipTürkiye Bilimsel ve Teknolojik Araştirma Kurumu, TÜBITAK, (TBAG-107T348)
dc.description.sponsorshipTürkiye Bilimsel ve Teknolojik Araştirma Kurumu, TÜBITAK
dc.identifier.doi10.3109/14756366.2011.574131
dc.identifier.eissn1475-6374
dc.identifier.endpage50
dc.identifier.issn1475-6374
dc.identifier.issue1
dc.identifier.pmid21635211
dc.identifier.scopus2-s2.0-79959914230
dc.identifier.startpage43
dc.identifier.urihttps://rdlopen.rawdatalibrary.net/r/bayburt/13975
dc.identifier.volume27
dc.identifier.wosWOS:000298748800008
dc.language.isoen
dc.publisherTAYLOR & FRANCIS LTD
dc.relation.ispartofJournal of Enzyme Inhibition and Medicinal Chemistry
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subjectBromophenols
dc.subjectCarbonic anhydrase
dc.subjectDiphenylmethane
dc.subjectEnzyme inhibition
dc.subjectGlaucoma
dc.subject.classificationBiochemistry & Molecular Biology
dc.subject.classificationChemistry, Medicinal
dc.subject.classificationPharmacology & Pharmacy
dc.subject.otherBenzophenones
dc.subject.otherBiological Agents
dc.subject.otherBromobenzenes
dc.subject.otherCarbonic Anhydrase II
dc.subject.otherCarbonic Anhydrase Inhibitors
dc.subject.otherCatechols
dc.subject.otherCytosol
dc.subject.otherDose-Response Relationship, Drug
dc.subject.otherHumans
dc.subject.otherIsoenzymes
dc.subject.otherMolecular Structure
dc.subject.otherStereoisomerism
dc.subject.otherStructure-Activity Relationship
dc.subject.other(2 bromo 3,4 dihydroxyphenyl)(2 bromo 4,5 dihydroxyphenyl)methanone
dc.subject.other(2 bromo 3,4 dihydroxyphenyl)(2,3 dibromo 4,5 dihydroxyphenyl)methanone
dc.subject.other(2 bromo 3,4 dimethoxyphenyl)(2 bromo 4,5 dimethoxyphenyl)methanone
dc.subject.other(2 bromo 3,4 dimethoxyphenyl)(2,3 dibromo 4,5 dimethoxyphenyl)methanone
dc.subject.other(2 bromo 3,4 dimethoxyphenyl)(3,4 dimethoxyphenyl)methanone
dc.subject.other(2 bromo 4,5 dihydroxyphenyl)(2,5 dibromo 3,4 dihydroxyphenyl)methanone
dc.subject.other(2 bromo 4,5 dihydroxyphenyl)(2,6 dibromo 3,4 dimethoxyphenyl)methanone
dc.subject.other(2 bromo 4,5 dimethoxyphenyl)(2,5 dibromo 3,4 dimethoxyphenyl)methanone
dc.subject.other(2 bromo 4,5 dimethoxyphenyl)(2,6 dibromo 3,4 dimethoxyphenyl)methanone
dc.subject.other3,4,6 tribromo 5 (2,5 dibromo 3,4 dihydroxybenzyl)benzene 1,2 diol
dc.subject.other5,5' methylene bis(3,4,6 tribromo benzene 1,2 diol)
dc.subject.otherbromine derivative
dc.subject.otherbromophenol blue
dc.subject.othercarbonate dehydratase II
dc.subject.othercarbonate dehydratase inhibitor
dc.subject.otherunclassified drug
dc.subject.otherarticle
dc.subject.otherbromination
dc.subject.otherdemethylation
dc.subject.otherdrug synthesis
dc.subject.otherenzyme inhibition
dc.subject.otherhuman
dc.subject.otherIC 50
dc.subject.otherpriority journal
dc.titleSynthesis and carbonic anhydrase inhibitory properties of novel bromophenols including natural products
dc.typeArticle
rdl.citation.openalex41
rdl.citation.scopus42
rdl.citation.wos43
rdl.oa.statusbronze
rdl.oa.urlhttps://www.tandfonline.com/doi/pdf/10.3109/14756366.2011.574131?needAccess=true
rdl.scopus.quartileQ2
rdl.sdgSDG03
rdl.source.indexSCOPUS
rdl.source.indexWOS
rdl.wos.indexScience Citation Index Expanded (SCI-EXPANDED)