Design and synthesis of new donepezil analogs derived from arylpiperazine scaffold as acetylcholinesterase inhibitors

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dc.authorid0000-0002-5976-676X
dc.authorid0000-0003-1896-2729
dc.authorid0000-0001-6047-2796
dc.authorid0000-0002-0841-1299
dc.contributor.authorŞahin, Zafer
dc.contributor.authorBiltekin, Sevde Nur
dc.contributor.authorBülbül, Emre Fatih
dc.contributor.authorYurttaş, Leyla
dc.contributor.authorBerk, Barkın
dc.contributor.authorDemirayak, Şeref
dc.date.accessioned2021-03-18T06:57:27Z
dc.date.available2021-03-18T06:57:27Z
dc.date.issued2020
dc.departmentİstanbul Medipol Üniversitesi, Eczacılık Fakültesi, Eczacılık Meslek Bilimleri Bölümü, Farmasötik Kimya Ana Bilim Dalı
dc.departmentİstanbul Medipol Üniversitesi, Eczacılık Fakültesi, Temel Eczacılık Bilimleri Bölümü, Farmasötik Mikrobiyoloji Ana Bilim Dalı
dc.description.abstractNewly synthesized 4-substituted phenyl-2-(4-substituted phenylpiperazine-1-yl)thiazole derivatives (4a-v) were evaluated in terms of their acetylcholinesterase (AChE) inhibition activities. Twenty-two compounds were tested against AChE at six different concentrations that varied between 10(-4)and 10(-9) M. The concentrations that inhibited AChE were calculated between 1.15 and 3.45 mu M in seven compounds (4a,4b,4h,4l,4m,4q,4r). Compounds4m,4b, and4lrepresented 1.15, 1.31, 1.34 mu M (IC50) inhibitions, respectively. Although the inhibition values are lower than that of donepezil, they are considerable. Modeling studies of these analogs revealed similar positioning with donepezil, in which Ar-Ar interactions with Tyr337 and Trp 286 exist.
dc.identifier.citationŞahin, Z., Biltekin, S. N., Bülbül, E. F., Yurttaş, L., Berk, B. ve Demirayak, Ş. (2020). Design and synthesis of new donepezil analogs derived from arylpiperazine scaffold as acetylcholinesterase inhibitors. Phosphorus, Sulfur and Silicon and the Related Elements, 196(3), 283-293. https://dx.doi.org/10.1080/10426507.2020.1830773
dc.identifier.doi10.1080/10426507.2020.1830773
dc.identifier.endpage293
dc.identifier.issn1042-6507
dc.identifier.issn1563-5325
dc.identifier.issue3
dc.identifier.scopusqualityQ4
dc.identifier.startpage283
dc.identifier.urihttps://dx.doi.org/10.1080/10426507.2020.1830773
dc.identifier.urihttps://hdl.handle.net/20.500.12511/6615
dc.identifier.volume196
dc.identifier.wosqualityQ4
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.language.isoen
dc.publisherTaylor & Francis Ltd
dc.relation.ispartofPhosphorus, Sulfur and Silicon and the Related Elementsen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/embargoedAccess
dc.subjectThiazole
dc.subjectPiperazine
dc.subjectAnticholinesterase Activity
dc.subjectAcetylcholinesterase Inhibition
dc.subjectMolecular Modeling
dc.titleDesign and synthesis of new donepezil analogs derived from arylpiperazine scaffold as acetylcholinesterase inhibitors
dc.typeArticle

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