Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Review
. 2021 Oct;98(4):655-673.
doi: 10.1111/cbdd.13919. Epub 2021 Jul 26.

Deciphering the detailed structure-activity relationship of coumarins as Monoamine oxidase enzyme inhibitors-An updated review

Vishal Payyalot Koyiparambath  1 , Krishnendu Prayaga Rajappan  1 , T M Rangarajan  2 , Abdullah G Al-Sehemi  3 , Mehboobali Pannipara  3 , Vaishnav Bhaskar  1 , Aathira Sujathan Nair  1 , Sachithra Thazhathuveedu Sudevan  1 , Sunil Kumar  1 , Bijo Mathew  1
Affiliations
Review

Deciphering the detailed structure-activity relationship of coumarins as Monoamine oxidase enzyme inhibitors-An updated review

Vishal Payyalot Koyiparambath et al. Chem Biol Drug Des. 2021 Oct.

Abstract

In the last few years, Monoamine oxidase (MAO) have emerged as a target for the treatment of many neurodegenerative diseases including anxiety, depression, Alzheimer's, and Parkinson's diseases. The MAO inhibitors especially selective and reversible inhibitors of either of the isoenzymes (MAO-A & MAO-B) have been given more attention as both the form have different therapeutic properties and hence can be used for different neurological disorders. The lack of selective and reversible inhibitors available for both the enzymes and severity of the neuronal disorder in society have opened a new door to the researchers to carry out large and dedicated researches in this field. Among the several classes of the molecule as the inhibitors, coumarins hold a rank as a potent scaffold with its ease of synthesis, high therapeutic potential, and reversibility in inhibiting MAOs. The current review is an update of the research in the field that covers the works during the last six years (2014-2020) with a major focus on the SAR of the coumarin derivatives including synthetic, natural, and hybrids of coumarins with FDA-approved drugs.

Keywords: Alzheimer's disease; coumarin; monoamine oxidase; structure-activity relationship.

PubMed Disclaimer

References

REFERENCES

    1. Abu-Aisheh, M. N., Al-Aboudi, A., Mustafa, M. S., El-Abadelah, M. M., Ali, S. Y., Ul-Haq, Z., & Mubarak, M. S. (2019). Coumarin derivatives as acetyl- and butyrylcholinestrase inhibitors: An in vitro, molecular docking, and molecular dynamics simulations study. Heliyon, 5(4), e01552. https://doi.org/10.1016/j.heliyon.2019.e01552
    1. Al-Amiery, A. A., Al-Majedy, Y. K., Kadhum, A. A. H., & Mohamad, A. B. (2015). Novel macromolecules derived from coumarin: Synthesis and antioxidant activity. Scientific Reports, 5, 4-10. https://doi.org/10.1038/srep11825
    1. Annunziata, F., Pinna, C., Dallavalle, S., Tamborini, L., & Pinto, A. (2020). An overview of coumarin as a versatile and readily accessible scaffold with broad-ranging biological activities. International Journal of Molecular Sciences, 21(13), 1-83. https://doi.org/10.3390/ijms21134618
    1. Baek, S. C., Kang, M.-G., Park, J.-E., Lee, J. P., Lee, H., Ryu, H. W., Park, C. M., Park, D., Cho, M.-L., Oh, S.-R., & Kim, H. (2019). Osthenol, a prenylated coumarin, as a monoamine oxidase A inhibitor with high selectivity. Bioorganic and Medicinal Chemistry Letters, 29(6), 839-843. https://doi.org/10.1016/j.bmcl.2019.01.016
    1. Binda, C., Hubálek, F., Li, M., Herzig, Y., Sterling, J., Edmondson, D. E., & Mattevi, A. (2005). Binding of rasagiline-related inhibitors to human monoamine oxidases: A kinetic and crystallographic analysis. Journal of Medicinal Chemistry, 48(26), 8148-8154. https://doi.org/10.1021/jm0506266

Publication types

MeSH terms

LinkOut - more resources