dc.contributor.author | Şahin, Zafer | |
dc.contributor.author | Biltekin, Sevde Nur | |
dc.contributor.author | Bülbül, Emre Fatih | |
dc.contributor.author | Yurttaş, Leyla | |
dc.contributor.author | Berk, Barkın | |
dc.contributor.author | Demirayak, Şeref | |
dc.date.accessioned | 2021-03-18T06:57:27Z | |
dc.date.available | 2021-03-18T06:57:27Z | |
dc.date.issued | 2020 | en_US |
dc.identifier.citation | Şahin, 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 | en_US |
dc.identifier.issn | 1042-6507 | |
dc.identifier.issn | 1563-5325 | |
dc.identifier.uri | https://dx.doi.org/10.1080/10426507.2020.1830773 | |
dc.identifier.uri | https://hdl.handle.net/20.500.12511/6615 | |
dc.description.abstract | Newly 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. | en_US |
dc.language.iso | eng | en_US |
dc.publisher | Taylor & Francis Ltd | en_US |
dc.rights | info:eu-repo/semantics/embargoedAccess | en_US |
dc.subject | Thiazole | en_US |
dc.subject | Piperazine | en_US |
dc.subject | Anticholinesterase Activity | en_US |
dc.subject | Acetylcholinesterase Inhibition | en_US |
dc.subject | Molecular Modeling | en_US |
dc.title | Design and synthesis of new donepezil analogs derived from arylpiperazine scaffold as acetylcholinesterase inhibitors | en_US |
dc.type | article | en_US |
dc.relation.ispartof | Phosphorus, Sulfur and Silicon and the Related Elements | en_US |
dc.department | İstanbul Medipol Üniversitesi, Eczacılık Fakültesi, Eczacılık Meslek Bilimleri Bölümü, Farmasötik Kimya Ana Bilim Dalı | en_US |
dc.department | İstanbul Medipol Üniversitesi, Eczacılık Fakültesi, Temel Eczacılık Bilimleri Bölümü, Farmasötik Mikrobiyoloji Ana Bilim Dalı | en_US |
dc.authorid | 0000-0002-5976-676X | en_US |
dc.authorid | 0000-0003-1896-2729 | en_US |
dc.authorid | 0000-0001-6047-2796 | en_US |
dc.authorid | 0000-0002-0841-1299 | en_US |
dc.identifier.volume | 196 | en_US |
dc.identifier.issue | 3 | en_US |
dc.identifier.startpage | 283 | en_US |
dc.identifier.endpage | 293 | en_US |
dc.relation.publicationcategory | Makale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı | en_US |
dc.identifier.doi | 10.1080/10426507.2020.1830773 | en_US |
dc.identifier.wosquality | Q4 | en_US |
dc.identifier.scopusquality | Q4 | en_US |