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2004
Enzyme inhibiting activity
X 0220
Synthesis and Evaluation of Tacrine-E2020 Hybrids as Acetylcholinesterase
for the Treatment of Alzheimer's Disease. — Tacrine-E2020 hybrids (I)
52- 211 Inhibitors
are potent AChE inhibitors, whereas the related compounds (IIb) and (IIc) are weak
inhibitors, and (IIa) reveals tacrine-like AChE inhibition. However, the selectivity of
related compounds (II) for AChE is higher than the selectivity of tacrine. Optimum
hybrid (Ib) has nanomolar affinity for AChE and is 37-fold more potent and 31-fold
more selective than tacrine. Modeling studies indicate that ligand (Ib) is nicely accommodated by AChE, engaging in appropriate hydrogen bond interactions. — (SHAO,
D.; ZOU, C.; LUO, C.; TANG, X.; LI*, Y.; Bioorg. Med. Chem. Lett. 14 (2004) 18,
4639-4642; Shanghai Inst. Mater. Med., Chin. Acad. Sci., Shanghai 200031,
Peop. Rep. China; Eng.) — H. Hoennerscheid
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