%0 Journal Article
%T Synthesis and acetylcholinesterase (AChE) inhibitory activity of some N -substituted-5-chloro-2(3 H )- benzoxazolone derivatives
%A Zeynep Soyer
%A Sulunay Parlar
%A Vildan Alptuzun
%J Marmara Pharmaceutical Journal
%D 2013
%I Marmara University Faculty of Pharmacy
%X Alzheimer¡¯s disease is a progressive neurodegenerative disorder of the central nervous system. Acetylcholinesterase inhibition is one of the proposed mechanisms for treatment of Alzheimer¡¯s disease. Currently, acetylcholinesterase inhibitors such as tacrine,donepezil, rivastigmine and galantamine are applied in different stages of Alzheimer¡¯s disease teratment. In recent years, various heterocyclic systems have been used as a skeletonto discover new acetylcholinesterase inhibitors. On the other hand, it is known that the benzoxazolone heterocyclic structure exhibited a wide range of biological activities. In this study, a seriesN-substituted-5-chloro-2(3H)-benzoxazolone derivatives were synthesized and evaluated their acetylcholinesterase inhibitory activity. These compounds were synthesized by Mannich reaction of 5-chloro-2(3H)-benzoxazolone with the appropriated amines.The acetylcholinesterase inhibitory activity of the title compounds was determined by colorimetric Ellman¡¯s method. The preliminary screening results indicated that 5-chloro-2-(3H)-benzoxazolone scaffold demonstrated different inhibition range againstacetylcholinesterase enzyme depending on the structural differences
%K acetylcholinesterase Inhibitory activity
%K 2(3 H )-benzoxazolone
%K mannich reac-tion
%K Ellman¡¯s method
%K synthesis.
%U http://www.marmaraeczacilikdergisi.com/pdf/pdf_MPJ_309.pdf