Acetyl- and butyrylcholinesterase inhibitory activity of selected photochemically synthesized polycycles

Authors : İvana SAGUD, İrena SKORIC, Dragana VUK, Ana RATKOVIC, Franko BURCUL

Pages : 1170-1182

View : 16 | Download : 10

Publication Date : 0000-00-00

Article Type : Research Paper

Abstract :Alzheimer`s disease insert ignore into journalissuearticles values(AD); is a progressive neurodegenerative disorder and the main cause of dementia in the elderly population. Since the treatment of AD has been associated with the activity of acetylcholinesterase insert ignore into journalissuearticles values(AChE); and butyrylcholinesterase insert ignore into journalissuearticles values(BChE);, their inhibitors remain the main focus of AD investigations. In this study we evaluated cholinesterase inhibitory activity of 14 bicyclo[3.2.1]octene/octadiene derivatives and naturally occurring sesquiterpene alcohol cedrol. These 14 compounds have been efficiently and ecologically prepared by a photochemical approach in batch photochemical reactors. Various compounds with the bicyclo[3.2.1]octene skeleton have already been successfully evaluated for treatment of central nervous system disorders and AD. Among the tested polycyclic derivatives, compounds 4-[insert ignore into journalissuearticles values(9$S);$-tricyclo[6.3.1.0$^{2,7}$]dodeca-2,4,6,10-tetraen-9-yl]pyridine insert ignore into journalissuearticles values(\textbf{3}); and insert ignore into journalissuearticles values(11$S);$-11-insert ignore into journalissuearticles values(4-chlorophenyl);-12-[insert ignore into journalissuearticles values($E);$-2-insert ignore into journalissuearticles values(4-chlorophenyl);ethenyl]tricyclo[6.3.1.0$^{2,7}$]dodeca-2,4,6,9-tetraene insert ignore into journalissuearticles values(\textbf{6}); showed the best inhibitory activity on BChE insert ignore into journalissuearticles values(IC$_{50}$ = 8.8 $\mu $M); and AChE insert ignore into journalissuearticles values(IC$_{50}$ = 17.5 $\mu $M);, respectively.
Keywords : Acetylcholinesterase inhibition, butyrylcholinesterase inhibition, benzobicyclo 3 2 1 octenes, benzobicyclo 3 2 1 octadienes, polycycles