TY - JOUR T1 - Synthesis and acetylcholinesterase (AChE) inhibitory activity of some N-substituted-5-chloro-2(3H)- benzoxazolone derivatives TT - Synthesis and acetylcholinesterase (AChE) inhibitory activity of some N-substituted-5-chloro-2(3H)- benzoxazolone derivatives AU - Soyer, Zeynep AU - Parlar, Sulunay AU - Alptuzun, Vildan PY - 2014 DA - March DO - 10.12991/mpj.61959 JF - Marmara Pharmaceutical Journal JO - J Res Pharm PB - Marmara University WT - DergiPark SN - 1309-0801 SP - 15 EP - 20 VL - 17 IS - 1 LA - en AB - ABSTRACT: Alzheimer’s disease is a progressive neurodegenerative disorder of the centralnervous system. Acetylcholinesterase inhibition is one of the proposed mechanisms fortreatment of Alzheimer’s disease. Currently, acetylcholinesterase inhibitors such as tacrine,donepezil, rivastigmine and galantamine are applied in different stages of Alzheimer’s diseaseteratment. 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 benzoxazoloneheterocyclic structure exhibited a wide range of biological activities. In thisstudy, a series N-substituted-5-chloro-2(3H)-benzoxazolone derivatives were synthesizedand evaluated their acetylcholinesterase inhibitory activity. These compounds were synthesizedby Mannich reaction of 5-chloro-2(3H)-benzoxazolone with the appropriated amines.The acetylcholinesterase inhibitory activity of the title compounds was determined by colorimetricEllman’s method. The preliminary screening results indicated that 5-chloro-2-(3H)-benzoxazolone scaffold demonstrated different inhibition range against acetylcholinesteraseenzyme depending on the structural differences.KEY WORDS: acetylcholinesterase Inhibitory activity, 2(3H)-benzoxazolone, mannich reaction,Ellman’s method, synthesis. 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