Synthesis of 5-substituted analogues of huperzine A |
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Authors: | Zhou G C Zhu D Y |
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Institution: | State Key Laboratory for Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, People's Republic of China. |
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Abstract: | Three 5-isosteres of huperzine A (2-4) were first synthesized. The key intermediate 10 was prepared by the reaction of acid 13 with LTA. The compounds 2 and 3 had 50% inhibition by 35 and 47 microM, respectively, which still retained antiacetylcholinesterase activity. |
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