What is the impact of structural modifications on the cholinesterase inhibitory activity of rivastigmine hybrids?

Label:chem

Topic
Cholinesterase inhibition is a key therapeutic strategy for AD, as it helps maintain acetylcholine levels in the brain. A study explored how structural modifications in rivastigmine hybrids affect their inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE).
Answer
A study found that adding an extra alkene group to the aromatic acid moiety in the hybrids (e.g., from 4AY3 to 4AY6) significantly enhanced AChE inhibitory activity. For instance, 4AY6 exhibited an IC50 value of 5 μM, compared to 110 μM for 4AY5. However, this modification had variable effects on BChE inhibition. The presence of catechol groups generally improved BChE inhibitory activity, with 4BY3 showing the most potent inhibitory activity (IC50 = 0.9 μM). The length of the linker between the rivastigmine and aromatic acid moieties also influenced activity, with shorter linkers generally showing better BChE inhibition.
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