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Huperzine-Based Derivatives: Design, Synthesis, and Anti-Alzheimer Activity

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Natural Product-based Synthetic Drug Molecules in Alzheimer's Disease

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Abstract

Alzheimer’s disease (AD) is a progressive illness of the nervous system typified by degenerative cognitive disability with challenging behavioural changes and dwindling physical activities for day-to-day living and remains one of the major reasons of dementia. As per the worldwide status report released by World Health Organization, the numbers of people with dementia will double every 20 years, reaching about 140 million in 2050. The currently used drugs for AD include galantamine, rivastigmine, and donepezil. These slow the progression of the disease or help to control cognitive and behavioural changes. Recently, aducanumab has been approved as a disease modifying drug targeting beta-amyloid and helps to reduce brain lesions. Another drug, memantine, is effective in regulating levels of glutamate, leading to brain cell death. Thus, the future involves multifunctional and targeted approaches, and multipotent naturally occurring agents have recently drawn attention in this regard. Huperzine A, derived from Huperzia serrata or Lycopodium serrata is one amongst these. Chemically, it is an alkaloid containing quinolizidine with good potency and selectivity and reversible inhibition of acetylcholinesterase. Many analogs of huperzine A have been reported but most of them are not able to cross the blood–brain barrier. Structural modifications of huperzine A are in process to achieve analogs with better anticholinesterase activity and improve their method of synthesis. The present chapter is aimed to compile and review the numerous evidence-based scientific information related to huperzine derivatives to make it easily available to the scientific community and researchers.

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Authors and Affiliations

  1. Dr. L. H. Hiranandani College of Pharmacy, University of Mumbai, Ulhasnagar, Maharashtra, India

    Vedika G. Dadlani & Harshal Ashok Pawar

  2. Institute of Pharmaceutical Sciences, University of Lucknow, Lucknow, Uttar Pradesh, India

    Pushpendra K. Tripathi

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  1. Vedika G. Dadlani
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  2. Harshal Ashok Pawar
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  3. Pushpendra K. Tripathi
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Editors and Affiliations

  1. Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research, Raebareli, Uttar Pradesh, India

    Abha Sharma

  2. Department of Pharmaceutical Engineering and Technology, Indian Institute of Technology BHU, Varanasi, Uttar Pradesh, India

    Gyan Prakash Modi

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Dadlani, V.G., Pawar, H.A., Tripathi, P.K. (2023). Huperzine-Based Derivatives: Design, Synthesis, and Anti-Alzheimer Activity. In: Sharma, A., Modi, G.P. (eds) Natural Product-based Synthetic Drug Molecules in Alzheimer's Disease. Springer, Singapore. https://doi.org/10.1007/978-981-99-6038-5_9

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  • DOI: https://doi.org/10.1007/978-981-99-6038-5_9

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