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Huperzine A, A Potential Therapeutic Agent for Treatment of Alzheimer's Disease

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HupA is a potent, reversible and selective inhibitor of AChE with a rapid absorption and penetration into the brain in animal tests. It exhibits memory-enhancing activities in animal and clinical trials. Compared to tacrine and donepezil, HupA possesses a longer duration of action and higher therapeutic index, and the peripheral cholinergic side effects are minimal at therapeutic doses. This review article deals with a comprehensive survey of the progress in chemical and pharmacological studies of HupA including the isolation and structure elucidation, pharmacological actions, total synthesis, SAR studies and the future development of HupA.

Recently, it has been reported that HupA could reduce neuronal cell death caused by glutamate. The dual bio-activities of HupA would further enhance its value and potentiality as the therapeutic agent for Alzheimers disease.
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Keywords: HupA; Huperzia serrata; SAR studies; alzheimer s disease; brain receptor; chiral catalyst; cyvlohexanedione mono ethylene ketal 10; diastereomeric separation; dimethyl 4 oxopimelate; donepezil; dual bio activities; enantiomer excess; enantioselective palladium catalyzed bicycloannula; entgegen; glutamate; huperzine A; inhibitor of AChE; keto ester; learning; lithium aluminium hydride; lycopoduim; memory; natura HupA; neuronal cell death; pharmacological actions; pyridine derivatives; recemic HupA; rectus; revesibile inhibitors if AChE; sinister left; stereiselective michael aldok reaction; structure activity relationships; structure elucidation; tetramethylguanidine; the anti AChE activities; total synthesis; zusammen together

Document Type: Review Article

Publication date: March 1, 2000

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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