New bisquaternary isoquinolinium inhibitors of brain cholinesterases - synthesis and anticholinesterase activity
2010
Abstract
Twelve bisquaternary isoquinolinium derivatives differing in the linker between two heteroarenium rings were synthesized and tested for their potency to inhibit brain cholinesterases. Anticholinesterase activity grew up with lenght of the connecting chain.
Possible binding to the enzyme cavity was described using software Autodock. LogP and molecular volume of prepared compounds were predicted.
The highest probability of synthesized compounds to penetrate blood-brain barrier could be expected for the compound with the linker having eight methylenes.