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compound 8i
- Development stage
- Preclinical
- Modality
- Small Molecules
01
Overview
Compound 8i is a novel small molecule inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) developed as a potential treatment for Alzheimer's disease. It acts as a dual-site inhibitor, binding simultaneously to the peripheral anionic site (PAS) and the catalytic active site (CAS) of both enzymes. In preclinical studies, compound 8i demonstrated potent inhibitory activity with IC50 values of 0.39 μM for AChE and 0.28 μM for BChE. Notably, it exhibited lower cytotoxicity compared to tacrine, suggesting a favorable safety profile for further development as a multipotent anti-Alzheimer's agent.
02
Targets
ButyrylcholinesteraseAcetylcholinesterase
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