دورية أكاديمية
Design and discovery of Novel Thiazole acetamide derivatives as anticholinesterase agent for possible role in the management of Alzheimer's.
| العنوان: | Design and discovery of Novel Thiazole acetamide derivatives as anticholinesterase agent for possible role in the management of Alzheimer's. |
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| المؤلفون: | Sun ZQ; Department of Internal Neurology, Linyi People's Hospital, No. 27, Jiefang Road, Linyi, Shandong 276000, PR China., Tu LX; Department of Internal Neurology, Linyi People's Hospital, No. 27, Jiefang Road, Linyi, Shandong 276000, PR China., Zhuo FJ; Department of Internal Neurology, Linyi People's Hospital, No. 27, Jiefang Road, Linyi, Shandong 276000, PR China., Liu SX; Department of Internal Neurology, Linyi People's Hospital, No. 27, Jiefang Road, Linyi, Shandong 276000, PR China. Electronic address: liusongxia@hotmail.com. |
| المصدر: | Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2016 Feb 01; Vol. 26 (3), pp. 747-750. Date of Electronic Publication: 2016 Jan 04. |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: Elsevier Science Ltd Country of Publication: England NLM ID: 9107377 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3405 (Electronic) Linking ISSN: 0960894X NLM ISO Abbreviation: Bioorg Med Chem Lett Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: Oxford : Elsevier Science Ltd Original Publication: Oxford ; New York : Pergamon Press, c1991- |
| مواضيع طبية MeSH: | Drug Design*, Acetamides/*chemistry , Cholinesterase Inhibitors/*chemistry , Thiazoles/*chemistry, Acetamides/pharmacology ; Acetamides/therapeutic use ; Acetylcholinesterase/chemistry ; Acetylcholinesterase/metabolism ; Alzheimer Disease/drug therapy ; Amyloid Precursor Protein Secretases/chemistry ; Amyloid Precursor Protein Secretases/metabolism ; Amyloid beta-Peptides/chemistry ; Amyloid beta-Peptides/metabolism ; Binding Sites ; Butyrylcholinesterase/chemistry ; Butyrylcholinesterase/metabolism ; Cell Survival/drug effects ; Cholinesterase Inhibitors/pharmacology ; Cholinesterase Inhibitors/therapeutic use ; Drug Evaluation, Preclinical ; HeLa Cells ; Humans ; Inhibitory Concentration 50 ; Molecular Docking Simulation ; Protein Binding ; Protein Structure, Tertiary ; Structure-Activity Relationship |
| مستخلص: | A novel series of thiazole acetamides was synthesized in excellent yields and characterized with the aid of various spectroscopic and elemental analysis. These compounds were evaluated for in vitro acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities for possible benefit in Alzheimers disease (AD). Among the synthesized compound, 6d was identified as the most potent compound of AChE (IC50=3.14±0.16 μM) with a selectivity index (SI) of 2.94 against BuChE. These compounds were further tested for inhibition of Aβ aggregation and β-secretase, where it showed potent inhibition which confirmed its multifactorial benefits in AD. The toxicity and docking study were also carried out to exemplify the pharmacological profile of compound 6d as prospective lead molecule against AD. (Copyright © 2016. Published by Elsevier Ltd.) |
| فهرسة مساهمة: | Keywords: Acetylcholinesterase; Docking; Synthesis; Thiazole acetamides |
| المشرفين على المادة: | 0 (Acetamides) 0 (Amyloid beta-Peptides) 0 (Cholinesterase Inhibitors) 0 (Thiazoles) EC 3.1.1.7 (Acetylcholinesterase) EC 3.1.1.8 (Butyrylcholinesterase) EC 3.4.- (Amyloid Precursor Protein Secretases) |
| تواريخ الأحداث: | Date Created: 20160120 Date Completed: 20161013 Latest Revision: 20171116 |
| رمز التحديث: | 20240628 |
| DOI: | 10.1016/j.bmcl.2016.01.001 |
| PMID: | 26783181 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 1464-3405 |
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| DOI: | 10.1016/j.bmcl.2016.01.001 |