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

[摘要]：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 H-1, C-13, and F-19 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.

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