Novel carvacrol based new oxypropanolamine derivatives: Design, synthesis, characterization, biological evaluation, and molecular docking studies

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dc.authoridTUZUN, BURAK/0000-0002-0420-2043
dc.authoridGulcin, ilhami/0000-0001-5993-1668
dc.authoridBytyqi-Damoni, Arlinda/0000-0002-9286-5487
dc.authoridZengin, Mustafa/0000-0002-0243-1432
dc.authoridGenc Bilgicli, Hayriye/0000-0001-6909-316X
dc.authoridTaslimi, Parham/0000-0002-3171-0633
dc.contributor.authorBytyqi-Damoni, Arlinda
dc.contributor.authorKestane, Ali
dc.contributor.authorTaslimi, Parham
dc.contributor.authorTuzun, Burak
dc.contributor.authorZengin, Mustafa
dc.contributor.authorBilgicli, Hayriye Genc
dc.contributor.authorGulcin, Ilhami
dc.date.accessioned2024-10-26T18:09:57Z
dc.date.available2024-10-26T18:09:57Z
dc.date.issued2020
dc.departmentSivas Cumhuriyet Üniversitesi
dc.description.abstractCarvacrol, as a natural product used for many years in the treatment of various diseases, therefore it was chosen as the starting compound for this study. Novel carvacrol based new oxypropanolamine derivatives were synthesized and characterized by spectroscopic methods. All new compounds were tested as metabolic enzyme inhibitory agents. Their clinical usage of carvacrol has been established as diuretics, antiepileptics, and anti-glaucoma factors, in the management of gastric, duodenal ulcers, mountain sickness, osteoporosis, idiopathic intracranial hypertension, or neurological disorders. The in vitro anti-hyperglycemic screening results showed that the compound 3d exhibits the maximum inhibitory effect against alpha-glycosidase enzyme (IC50: 904.10 nM). In addition, the compounds 3d (IC50: 29.74 nM and 23.64 nM) and 3e (IC50: 31.28 nM and 26.11 nM) were found to have a significant response to inhibit carbonic anhydrase I, and II isoenzymes (hCA I and II), respectively. The novel carvacrol based oxypropanolamine compounds were effective inhibitors of the hCA I and II isozymes, and acetylcholinesterase with Ki values in the range of 27.18-44.84 nM for hCA I, 25.62-38.71 nM for hCA II, and 99.83-146.25 nM for AChE, respectively. (C) 2019 Elsevier B.V. All rights reserved.y
dc.identifier.doi10.1016/j.molstruc.2019.127297
dc.identifier.issn0022-2860
dc.identifier.issn1872-8014
dc.identifier.scopus2-s2.0-85074416116
dc.identifier.scopusqualityQ2
dc.identifier.urihttps://doi.org/10.1016/j.molstruc.2019.127297
dc.identifier.urihttps://hdl.handle.net/20.500.12418/30360
dc.identifier.volume1202
dc.identifier.wosWOS:000501486700066
dc.identifier.wosqualityQ3
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.language.isoen
dc.publisherElsevier
dc.relation.ispartofJournal of Molecular Structure
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.subjectOxypropanolamine
dc.subjectAcetylcholinesterase
dc.subjectCarbonic anhydrase
dc.subjectEnzyme inhibition
dc.subjectMolecular docking
dc.titleNovel carvacrol based new oxypropanolamine derivatives: Design, synthesis, characterization, biological evaluation, and molecular docking studies
dc.typeArticle

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