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Synthesis of 1‐[(1R)‐1‐(6‐fluoro‐1,3‐benzothiazol‐2‐yl)ethyl]‐3‐substituted phenyl ureas and their inhibition activity to acetylcholinesterase and butyrylcholinesterase
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2010-09-02 , DOI: 10.1002/jhet.502
Vladimír Pejchal , Šárka Štěpánková , Pavel Drabina

A series of novel 1‐[(1R)‐1‐(6‐fluoro‐1,3‐benzothiazol‐2‐yl)ethyl]‐3‐substituted phenyl ureas were synthesized by the condensation of (1R)‐1‐(6‐fluoro‐1,3‐benzothiazol‐2‐yl)ethanamine with substituted phenyl isocyanates under mild conditions. Their structures were confirmed 1H, 13C, and 19F NMR spectra, and elemental analyses. The optical activities were confirmed by optical rotation measurements. The inhibition activity of 1‐[(1R)‐1‐(6‐fluoro‐1,3‐benzothiazol‐2‐yl)ethyl]‐3‐substituted phenyl ureas to acetylcholinesterase (ACHE) and butyrylcholinesterase (BCHE) was also tested. Preliminary bioassay indicated that the target ureas displayed excellent acetylcholinesterase and butyrylcholinesterase inhibition activity. J. Heterocyclic Chem., 2011.

中文翻译:

1-[(1R)-1-(6-氟-1,3-苯并噻唑-2-基)乙基] -3-取代的苯基脲的合成及其对乙酰胆碱酯酶和丁酰胆碱酯酶的抑制活性

一系列新颖的1 - [(1 - [R)-1-(6-氟-1,3-苯并噻唑-2-基)乙基] -3 -取代的苯基脲由(1的缩合合成- [R)-1- (6-氟-1,3-苯并噻唑-2-基)乙胺与取代的异氰酸苯酯在温和的条件下。通过1 H,13 C和19 F NMR光谱以及元素分析确认了它们的结构。通过旋光度测量确认光学活性。1 – [(1 R还测试了)-1-(6-氟-1,3-苯并噻唑-2-基)乙基] -3-取代的苯基脲与乙酰胆碱酯酶(ACHE)和丁酰胆碱酯酶(BCHE)的关系。初步的生物测定表明,目标尿素显示出优异的乙酰胆碱酯酶和丁酰胆碱酯酶抑制活性。J.杂环化​​学.2011。
更新日期:2010-09-02
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