Synthesis and acetylcholinesterase (AChE) inhibitory activity of some N-substituted-5-chloro-2(3H)- benzoxazolone derivatives
Makaleler > Tam Makale · 2014
Yazarlar: Zeynep SOYER, Sülünay PARLAR ÇOŞKUN, Vildan ALPTÜZÜN
Dspace Repository (Marmara Üniversitesi), Uluslararası, 2014
DOI: 10.12991/mpj.61959
Özet
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.