Synthesis, characterisation, biological evaluation and in silico studies of sulphonamide Schiff bases

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dc.authoridDURGUN, Mustafa/0000-0003-3012-7582
dc.authoridakocak, suleyman/0000-0003-4506-5265
dc.authoridDemir, Yeliz/0000-0003-3216-1098
dc.authoridkuru, ali/0000-0002-8300-1572
dc.authoridIşık, Mesut/0000-0002-4677-8104
dc.authoridOsman, Sameh/0000-0003-1564-7301
dc.authoridGÜZEL, Abdussamat/0000-0001-7810-4510
dc.authorwosidDURGUN, Mustafa/AAG-4570-2019
dc.authorwosidGUZEL, ABDUSSAMAT/AAI-1866-2019
dc.authorwosidakocak, suleyman/AAU-8087-2020
dc.authorwosidDemir, Yeliz/ABI-5719-2020
dc.authorwosidkuru, ali/HLG-9953-2023
dc.authorwosidIşık, Mesut/ABG-4558-2020
dc.authorwosidTürkeş, Cüneyt/AAC-7338-2021
dc.contributor.authorDurgun, Mustafa
dc.contributor.authorTurkes, Cuneyt
dc.contributor.authorIsik, Mesut
dc.contributor.authorDemir, Yeliz
dc.contributor.authorSakli, Ali
dc.contributor.authorKuru, Ali
dc.contributor.authorGuzel, Abdussamat
dc.date.accessioned2024-08-04T20:47:14Z
dc.date.available2024-08-04T20:47:14Z
dc.date.issued2020
dc.departmentİnönü Üniversitesien_US
dc.description.abstractSulphonamides are biologically important compounds with low toxicity, many bioactivities and cost-effectiveness. Eight sulphonamide derivatives were synthesised and characterised by FT-IR, C-13 NMR, H-1 NMR, LC-MS and elemental analysis. Their inhibitory effect on AChE, and carbonic anhydrase I and II enzyme activities was investigated. Their antioxidant activity was determined using different bioanalytical assays such as radical scavenging tests with ABTS(center dot+), and DPPH center dot+ as well as metal-reducing abilities with CUPRAC, and FRAP assays. All compounds showed satisfactory enzyme inhibitory potency in nanomolar concentrations against AChE and CA isoforms with K-I values ranging from 10.14 +/- 0.03 to 100.58 +/- 1.90 nM. Amine group containing derivatives showed high metal reduction activity and about 70% ABTS radical scavenging activity. Due to their antioxidant activity and AChE inhibition, these novel compounds may be considered as leads for investigations in neurodegenerative diseases.en_US
dc.description.sponsorshipKing Saud University, Riyadh, Saudi Arabia [RSP-2019/1]en_US
dc.description.sponsorshipThis work was in part also funded by the Researchers Supporting Project No. (RSP-2019/1) King Saud University, Riyadh, Saudi Arabia.en_US
dc.identifier.doi10.1080/14756366.2020.1746784
dc.identifier.endpage962en_US
dc.identifier.issn1475-6366
dc.identifier.issn1475-6374
dc.identifier.issue1en_US
dc.identifier.pmid32249705en_US
dc.identifier.scopus2-s2.0-85083022713en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.startpage950en_US
dc.identifier.urihttps://doi.org/10.1080/14756366.2020.1746784
dc.identifier.urihttps://hdl.handle.net/11616/99245
dc.identifier.volume35en_US
dc.identifier.wosWOS:000523492900001en_US
dc.identifier.wosqualityQ1en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherTaylor & Francis Ltden_US
dc.relation.ispartofJournal of Enzyme Inhibition and Medicinal Chemistryen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.subjectAcetylcholinesteraseen_US
dc.subjectcarbonic anhydraseen_US
dc.subjectsynthesisen_US
dc.subjectsulphonamideen_US
dc.subjectmolecular dockingen_US
dc.titleSynthesis, characterisation, biological evaluation and in silico studies of sulphonamide Schiff basesen_US
dc.typeArticleen_US

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