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Coumarin and Its Derivatives III
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Coumarin and Its Derivatives III

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Natural Products Chemistry".

Deadline for manuscript submissions: closed (31 July 2024) | Viewed by 1794

Special Issue Editor

Dr. Maria João Matos

E-Mail Website
Guest Editor
Department of Organic Chemistry, Faculty of Pharmacy, University of Santiago de Compostela, 15782 Santiago de Compostela, Spain
Interests: coumarins; natural product chemistry; organic chemistry; medicinal chemistry; chemical biology; computational chemistry
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Coumarin is a privileged scaffold in medicinal chemistry. Its derivatives are widely distributed in nature and can be found in a large number of naturally occurring and synthetic bioactive molecules. This scaffold is a unique and versatile oxygen-containing heterocyclic structure, presenting a large conjugated system with electron-rich and charge transport properties. These properties are responsible for the interaction of this scaffold with other molecules, such as biomolecules and ions. Therefore, a great number of coumarin derivatives have been designed, synthetized, and evaluated against different pharmacological targets. In addition, coumarin-based ion receptors, fluorescent probes, and biological stains are growing quickly and have extensive applications with which to monitor enzyme activity and complex biological events in a timely manner, as well as accurately monitor pharmacological and pharmacokinetic properties in living cells. The extraction, synthesis, and biological evaluation of coumarins have become extremely attractive and rapidly developing topics. Research articles, reviews, communications, and concept papers focused on the multidisciplinary profile of coumarins, highlighting natural sources, most recently synthetic pathways, along with the main biological applications and theoretical studies, are welcome for this Special Issue.

Dr. Maria João Matos
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

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Keywords

  • coumarins
  • natural products
  • synthesis
  • bioactivity
  • fluorescent dyes
  • computational studies
  • analytical methods
  • medicinal chemistry
  • chemical biology
  • drug discovery

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Related Special Issues

Published Papers (2 papers)

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Research

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9 pages, 3148 KiB  
Article
Novel Dihydrocoumarins Induced by Radiolysis as Potent Tyrosinase Inhibitors
by Gyeong Han Jeong, Manisha Yadav, Seung Sik Lee, Byung Yeoup Chung, Jae-Hyeon Cho, In-Chul Lee, Hyoung-Woo Bai and Tae Hoon Kim
Molecules 2024, 29(2), 341; https://doi.org/10.3390/molecules29020341 - 10 Jan 2024
Viewed by 902
Abstract
A representative naturally occurring coumarin, 4-methylumbelliferone (5), was exposed to 50 kGy of gamma ray, resulting in four newly generated dihydrocoumarin products 1–4 induced by the gamma irradiation. The structures of these new products were elucidated by interpretation of [...] Read more.
A representative naturally occurring coumarin, 4-methylumbelliferone (5), was exposed to 50 kGy of gamma ray, resulting in four newly generated dihydrocoumarin products 1–4 induced by the gamma irradiation. The structures of these new products were elucidated by interpretation of spectroscopic data (NMR, MS, [α]D, and UV). The unusual bisdihydrocoumarin 4 exhibited improved tyrosinase inhibitory capacity toward mushroom tyrosinase with IC50 values of 19.8 ± 0.5 μM as compared to the original 4-methylumbelliferone (5). A kinetic analysis also exhibited that the potent metabolite 4 had non-competitive modes of action. Linkage of the hydroxymethyl group in the C-3 and C-4 positions on the lactone ring probably enhances the tyrosinase inhibitory effect of 4-methylumbelliferone (5). Thus, the novel coumarin analog 4 is an interesting new class of tyrosinase inhibitory candidates that requires further examination. Full article
(This article belongs to the Special Issue Coumarin and Its Derivatives III)
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Review

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24 pages, 4777 KiB  
Review
Naturally Inspired Coumarin Derivatives in Alzheimer’s Disease Drug Discovery: Latest Advances and Current Challenges
by Rebecca Orioli, Federica Belluti, Silvia Gobbi, Angela Rampa and Alessandra Bisi
Molecules 2024, 29(15), 3514; https://doi.org/10.3390/molecules29153514 - 26 Jul 2024
Viewed by 477
Abstract
The main feature of neurodegenerative diseases, including Alzheimer’s disease, is the network of complex and not fully recognized neuronal pathways and targets involved in their onset and progression. The therapeutic treatment, at present mainly symptomatic, could benefit from a polypharmacological approach based on [...] Read more.
The main feature of neurodegenerative diseases, including Alzheimer’s disease, is the network of complex and not fully recognized neuronal pathways and targets involved in their onset and progression. The therapeutic treatment, at present mainly symptomatic, could benefit from a polypharmacological approach based on the development of a single molecular entity designed to simultaneously modulate different validated biological targets. This strategy is principally based on molecular hybridization, obtained by linking or merging different chemical moieties acting with synergistic and/or complementary mechanisms. The coumarin core, widely found in nature, endowed with a recognized broad spectrum of pharmacological activities, large synthetic accessibility and favourable pharmacokinetic properties, appears as a valuable, privileged scaffold to be properly modified in order to obtain compounds able to engage different selected targets. The scientific literature has long been interested in the multifaceted profiles of coumarin derivatives, and in this review, a survey of the most important results of the last four years, on both natural and synthetic coumarin-based compounds, regarding the development of anti-Alzheimer’s compounds is reported. Full article
(This article belongs to the Special Issue Coumarin and Its Derivatives III)
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