New PEPPSI-Pd-NHC complexes bearing 4-hydroxyphenylethyl group: Synthesis, characterization, molecular docking, and bioactivity properties

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dc.authoridTASKIN TOK, Tugba/0000-0002-0064-8400
dc.authoridAktaş, Aydın/0000-0001-8496-6782
dc.authoridGulcin, ilhami/0000-0001-5993-1668
dc.authoridTaslimi, Parham/0000-0002-3171-0633
dc.authorwosidTASKIN TOK, Tugba/A-8885-2016
dc.authorwosidTaslimi, Parham/AAL-2788-2020
dc.authorwosidAktaş, Aydın/J-6194-2019
dc.authorwosidGulcin, ilhami/F-1428-2014
dc.contributor.authorBehcet, Ayten
dc.contributor.authorTaslimi, Parham
dc.contributor.authorGok, Yetkin
dc.contributor.authorAktas, Aydin
dc.contributor.authorTaskin-Tok, Tugba
dc.contributor.authorGulcin, Ilhami
dc.date.accessioned2024-08-04T20:52:15Z
dc.date.available2024-08-04T20:52:15Z
dc.date.issued2022
dc.departmentİnönü Üniversitesien_US
dc.description.abstractFive 4-hydroxyphenylethyl substituted pyridine enhanced, precatalyst, preparation, stabilization, and initiation-Pd-N-heterocyclic carbene (PEPPSI-Pd-NHC) complexes are synthesized in a straightforward way. All PEPPSI-Pd-NHC complexes were prepared by mixing 4-hydroxyphenylethyl substituted NHC precursors, palladium chloride, potassium carbonate, and potassium bromide in pyridine. All complexes were screened for human carbonic anhydrase I (hCA I) and hCA II, acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and alpha-glucosidase (alpha-Glu) inhibitory activities. The ChE inhibitory activities of the new PEPPSI-Pd-NHC complexes bearing the 4-hydroxyphenylethyl group (12-e) against alpha-Glu, AChE, and BChE were determined by the Tao and Ellman methods. The results indicated that all the synthetic complexes exhibited potent inhibitory activities against all targets as compared to the standard inhibitors, revealed by IC50 values. The K-i values of the new PEPPSI-Pd-NHC complexes 1a-e for hCA I, hCA II, AChE, BChE, and alpha-Glu were obtained in the ranges of 18.98-32.65, 22.95-38.13, 3.67-11.65, 4.09-9.36, 186.92-287.45 mu M, respectively. Among the synthesized complexes, the most potent complexes were 1c toward hCA I and II with K-i values 18.98 and 22.95 mu M, and 1d toward AChE and BChE with K-i = 3.67 and 4.09 mu M, respectively.en_US
dc.description.sponsorshipBartin Universitesi [2020-FEN-B-005]en_US
dc.description.sponsorshipBartin Universitesi, Grant/Award Number: 2020-FEN-B-005en_US
dc.identifier.doi10.1002/ardp.202200276
dc.identifier.issn0365-6233
dc.identifier.issn1521-4184
dc.identifier.issue12en_US
dc.identifier.pmid35986370en_US
dc.identifier.scopus2-s2.0-85136468031en_US
dc.identifier.scopusqualityQ2en_US
dc.identifier.urihttps://doi.org/10.1002/ardp.202200276
dc.identifier.urihttps://hdl.handle.net/11616/100854
dc.identifier.volume355en_US
dc.identifier.wosWOS:000842312100001en_US
dc.identifier.wosqualityQ1en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherWiley-V C H Verlag Gmbhen_US
dc.relation.ispartofArchiv Der Pharmazieen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectalpha-glucosidaseen_US
dc.subjectenzyme inhibitionen_US
dc.subjectmolecular dockingen_US
dc.subjectNHC complexesen_US
dc.subjectPEPPSIen_US
dc.titleNew PEPPSI-Pd-NHC complexes bearing 4-hydroxyphenylethyl group: Synthesis, characterization, molecular docking, and bioactivity propertiesen_US
dc.typeArticleen_US

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