Potent, easily synthesized huperzine A-tacrine hybrid acetylcholinesterase inhibitors. |
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| Authors: | P R Carlier D M Du Y Han J Liu Y P Pang |
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| Affiliation: | Department of Chemistry, Hong Kong University of Science and Technology, Clear Water Bay, Kowloon. chpaul@ust.hk |
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| Abstract: | Hybrid acetylcholinesterase inhibitors composed of a key fragment of huperzine A and an intact tacrine unit were prepared. The syntheses are quite direct, proceeding in a maximum of 4 linear steps from commercially available starting materials. The optimum hybrid inhibitor (+/-)-9g is 13-fold more potent than (-)-huperzine A, and 25-fold more potent than tacrine. |
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