YYÜ GCRIS Basic veritabanının içerik oluşturulması ve kurulumu Research Ecosystems (https://www.researchecosystems.com) tarafından devam etmektedir. Bu süreçte gördüğünüz verilerde eksikler olabilir.
 

Mono- or Di-Substituted Imidazole Derivatives for Inhibition of Acetylcholine and Butyrylcholine Esterases

dc.authorid Gulcin, Ilhami/0000-0001-5993-1668
dc.authorid Taslimi, Parham/0000-0002-3171-0633
dc.authorid Menges, Nurettin/0000-0002-5990-6275
dc.authorscopusid 57170612000
dc.authorscopusid 57221383476
dc.authorscopusid 56658628800
dc.authorscopusid 35509141500
dc.authorscopusid 22235844100
dc.authorscopusid 23973608700
dc.authorwosid Taslimi, Parham/Aal-2788-2020
dc.authorwosid Taşpinar, Mehmet/Lig-3987-2024
dc.authorwosid Kuzu, Burak/Aae-1597-2022
dc.authorwosid Tan Uygun, Meltem/Aad-1641-2021
dc.authorwosid Gulcin, Ilhami/F-1428-2014
dc.authorwosid Menges, Nurettin/F-9678-2016
dc.contributor.author Kuzu, Burak
dc.contributor.author Tan, Meltem
dc.contributor.author Taslimi, Parham
dc.contributor.author Gulcin, Ilhami
dc.contributor.author Taspinar, Mehmet
dc.contributor.author Menges, Nurettin
dc.date.accessioned 2025-05-10T17:34:08Z
dc.date.available 2025-05-10T17:34:08Z
dc.date.issued 2019
dc.department T.C. Van Yüzüncü Yıl Üniversitesi en_US
dc.department-temp [Kuzu, Burak; Tan, Meltem; Menges, Nurettin] Van Yuzuncu Yil Univ, Pharmaceut Chem Sect, TR-65080 Van, Turkey; [Kuzu, Burak; Tan, Meltem; Menges, Nurettin] YYU TEKNOKENT, SAFF Chem Reagent R&D Lab, TR-65080 Van, Turkey; [Taslimi, Parham; Gulcin, Ilhami] Ataturk Univ, Dept Chem, TR-25240 Erzurum, Turkey; [Taspinar, Mehmet] Van Yuzuncu Yil Univ, Dept Med Biol, TR-65080 Van, Turkey en_US
dc.description Gulcin, Ilhami/0000-0001-5993-1668; Taslimi, Parham/0000-0002-3171-0633; Menges, Nurettin/0000-0002-5990-6275 en_US
dc.description.abstract Mono- or di-substituted imidazole derivatives were synthesized using a one-pot, two-step strategy. All imidazole derivatives were tested for AChE and BChE inhibition and showed nanomolar activity similar to that of the test compound donepezil and higher than that of tacrine. Structure activity relationship studies, docking studies to on X-ray crystal structure of AChE with PDB code 1B41, and adsorption, distribution, metabolism, and excretion (ADME) predictions were performed. The synthesized core skeleton was bound to important regions of the active site of AChE such as the peripheral anionic site (PAS), oxyanion hole (OH), and anionic subsite (AS). Selectivity of the reported test compounds was calculated and enzyme kinetic studies revealed that they behave as competitive inhibitors, while two of the test compounds showed noncompetitive inhibitory behavior. ADME predictions revealed that the synthesized molecules might pass through the blood brain barrier and intestinal epithelial barrier and circulate freely in the blood stream without binding to human serum albumin. While the toxicity of one compound on the WS1 (skin fibroblast) cell line was 1790 mu M, its toxicity on the SH-SY5Y (neuroblastoma) cell line was 950 mu M. en_US
dc.description.sponsorship Scientific and Technologic Research Agency of Turkey (TUBITAK) [115Z112, 115Z894] en_US
dc.description.sponsorship This study was partly funded by Scientific and Technologic Research Agency of Turkey (TUBITAK) (grant numbers: 115Z112, 115Z894) en_US
dc.description.woscitationindex Science Citation Index Expanded - Index Chemicus
dc.identifier.doi 10.1016/j.bioorg.2019.01.044
dc.identifier.endpage 196 en_US
dc.identifier.issn 0045-2068
dc.identifier.issn 1090-2120
dc.identifier.pmid 30711701
dc.identifier.scopus 2-s2.0-85060892582
dc.identifier.scopusquality Q1
dc.identifier.startpage 187 en_US
dc.identifier.uri https://doi.org/10.1016/j.bioorg.2019.01.044
dc.identifier.uri https://hdl.handle.net/20.500.14720/13710
dc.identifier.volume 86 en_US
dc.identifier.wos WOS:000464108100021
dc.identifier.wosquality Q1
dc.language.iso en en_US
dc.publisher Academic Press inc Elsevier Science en_US
dc.relation.publicationcategory Makale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı en_US
dc.rights info:eu-repo/semantics/closedAccess en_US
dc.subject Sar en_US
dc.subject Docking en_US
dc.subject Alzheimer'S Disease en_US
dc.subject Water Solubility en_US
dc.subject Adme en_US
dc.subject Enzyme Kinetic Study en_US
dc.title Mono- or Di-Substituted Imidazole Derivatives for Inhibition of Acetylcholine and Butyrylcholine Esterases en_US
dc.type Article en_US

Files