Analogues of tacrine were synthesized and evaluated for acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activity. Compound 2a was the most potent inhibitor of AChE with a higher selectivity than tacrine for AChE over BuChE. Tacrine, on the other hard, showed the opposite behaviour with a weaker inhibitory effect on AChE than on BuChe. The compounds displayed correlated activities in isolated enzymes as well as in rat brain homogenates. (C) 1997 Elsevier Science Ltd.
Acetylcholinesterase inhibition by tacrine analogues
GIUSTI, PIETRO
1997
Abstract
Analogues of tacrine were synthesized and evaluated for acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activity. Compound 2a was the most potent inhibitor of AChE with a higher selectivity than tacrine for AChE over BuChE. Tacrine, on the other hard, showed the opposite behaviour with a weaker inhibitory effect on AChE than on BuChe. The compounds displayed correlated activities in isolated enzymes as well as in rat brain homogenates. (C) 1997 Elsevier Science Ltd.
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