engleski

Acetyl- and butyrylcholinesterase inhibitory activity of selected photochemically synthesized polycycles

Alzheimer’s disease (AD) is a progressive neurodegenerative disorder and the main cause of dementia in elderly population. Since the treatment of AD has been associated with the activity of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) their inhibitors remain the main focus of AD investigations. In this study we evaluated cholinesterase inhibitory activity of fourteen bicyclo[3.2.1]octene/octadiene derivatives and naturally occurring sesquiterpene alcohol cedrol. These fourteen compounds have been efficiently and ecologically prepared by 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 (CNS) disorders and Alzheimer disease. Among the tested polycyclic derivatives, compounds 4-[(9S)- tricyclo[6.3.1.02, 7]dodeca-2, 4, 6, 10- tetraen-9- yl]pyridine (3) and (11S)-11-(4- chlorophenyl)-12-[(E)-2-(4- chlorophenyl)ethenyl]tricyclo[6.3.1.02, 7]dodeca- 2, 4, 6, 9-tetraene (6) showed the best inhibitory activity on BChE (IC50=8.8 μM) and AChE (IC50=17.5 μM), respectively.

acetylcholinesterase inhibition ; butyrylcholinesterase inhibition ; benzobicyclo[3.2.1]octenes ; benzobicyclo[3.2.1]octadienes ; polycycles

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