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Design and discovery of Novel Thiazole acetamide derivatives as anticholinesterase agent for possible role in the management of Alzheimer's.
Bioorg Med Chem Lett. 2016 Feb 01; 26(3):747-750.BM

Abstract

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.

Authors+Show Affiliations

Department of Internal Neurology, Linyi People's Hospital, No. 27, Jiefang Road, Linyi, Shandong 276000, PR China.Department of Internal Neurology, Linyi People's Hospital, No. 27, Jiefang Road, Linyi, Shandong 276000, PR China.Department of Internal Neurology, Linyi People's Hospital, No. 27, Jiefang Road, Linyi, Shandong 276000, PR China.Department of Internal Neurology, Linyi People's Hospital, No. 27, Jiefang Road, Linyi, Shandong 276000, PR China. Electronic address: liusongxia@hotmail.com.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

26783181

Citation

Sun, Zhi-Qing, et al. "Design and Discovery of Novel Thiazole Acetamide Derivatives as Anticholinesterase Agent for Possible Role in the Management of Alzheimer's." Bioorganic & Medicinal Chemistry Letters, vol. 26, no. 3, 2016, pp. 747-750.
Sun ZQ, Tu LX, Zhuo FJ, et al. Design and discovery of Novel Thiazole acetamide derivatives as anticholinesterase agent for possible role in the management of Alzheimer's. Bioorg Med Chem Lett. 2016;26(3):747-750.
Sun, Z. Q., Tu, L. X., Zhuo, F. J., & Liu, S. X. (2016). Design and discovery of Novel Thiazole acetamide derivatives as anticholinesterase agent for possible role in the management of Alzheimer's. Bioorganic & Medicinal Chemistry Letters, 26(3), 747-750. https://doi.org/10.1016/j.bmcl.2016.01.001
Sun ZQ, et al. Design and Discovery of Novel Thiazole Acetamide Derivatives as Anticholinesterase Agent for Possible Role in the Management of Alzheimer's. Bioorg Med Chem Lett. 2016 Feb 1;26(3):747-750. PubMed PMID: 26783181.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Design and discovery of Novel Thiazole acetamide derivatives as anticholinesterase agent for possible role in the management of Alzheimer's. AU - Sun,Zhi-Qing, AU - Tu,Li-Xiang, AU - Zhuo,Feng-Juan, AU - Liu,Song-Xia, Y1 - 2016/01/04/ PY - 2015/09/21/received PY - 2015/12/16/revised PY - 2016/01/04/accepted PY - 2016/1/20/entrez PY - 2016/1/20/pubmed PY - 2016/10/14/medline KW - Acetylcholinesterase KW - Docking KW - Synthesis KW - Thiazole acetamides SP - 747 EP - 750 JF - Bioorganic & medicinal chemistry letters JO - Bioorg Med Chem Lett VL - 26 IS - 3 N2 - 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. SN - 1464-3405 UR - https://www.unboundmedicine.com/medline/citation/26783181/Design_and_discovery_of_Novel_Thiazole_acetamide_derivatives_as_anticholinesterase_agent_for_possible_role_in_the_management_of_Alzheimer's_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0960-894X(16)30001-4 DB - PRIME DP - Unbound Medicine ER -