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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

✍ Scribed by Vladimír Pejchal; Šárka Štěpánková; Pavel Drabina

Publisher
Journal of Heterocyclic Chemistry
Year
2010
Tongue
English
Weight
121 KB
Volume
48
Category
Article
ISSN
0022-152X

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✦ Synopsis

Abstract

A series of novel 1‐[(1__R__)‐1‐(6‐fluoro‐1,3‐benzothiazol‐2‐yl)ethyl]‐3‐substituted phenyl ureas were synthesized by the condensation of (1__R__)‐1‐(6‐fluoro‐1,3‐benzothiazol‐2‐yl)ethanamine with substituted phenyl isocyanates under mild conditions. Their structures were confirmed ^1^H, ^13^C, and ^19^F NMR spectra, and elemental analyses. The optical activities were confirmed by optical rotation measurements. The inhibition activity of 1‐[(1__R__)‐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.

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## Abstract magnified image Synthesis of some novel 2‐{2‐[1‐(3‐substitutedphenyl)‐1__H__‐1,2, 3‐triazol‐4‐yl‐]ethyl)‐1__H__‐benzo[__d__]‐imidazole derivatives, by the condensation of o‐phenylenediamine with 3‐(1‐(3‐substituted‐phenyl)‐1__H__‐1,2,3‐triazol‐4‐yl) propanoic acid and then subsequent r