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Bioorg Med Chem Lett. 2016 Feb 1;26(3):747-750. doi: 10.1016/j.bmcl.2016.01.001. Epub 2016 Jan 4.

Design and discovery of Novel Thiazole acetamide derivatives as anticholinesterase agent for possible role in the management of Alzheimer's.

Author information

1
Department of Internal Neurology, Linyi People's Hospital, No. 27, Jiefang Road, Linyi, Shandong 276000, PR China.
2
Department of Internal Neurology, Linyi People's Hospital, No. 27, Jiefang Road, Linyi, Shandong 276000, PR China. Electronic address: liusongxia@hotmail.com.

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.

KEYWORDS:

Acetylcholinesterase; Docking; Synthesis; Thiazole acetamides

PMID:
26783181
DOI:
10.1016/j.bmcl.2016.01.001
[Indexed for MEDLINE]

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