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Molecules
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Recent Advances in the Organic Synthesis of Bioactive Compounds
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Recent Advances in the Organic Synthesis of Bioactive Compounds

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

Deadline for manuscript submissions: closed (30 November 2024) | Viewed by 5785

Special Issue Editors

Prof. Dr. José Justicia

E-Mail Website
Guest Editor
Department of Organic Chemistry, University of Granada, 18071 Granada, Spain
Interests: natural products; terpenoids; organic synthesis; free radicals; organometallic chemistry
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Rachid Chahboun

E-Mail Website
Guest Editor
Department of Organic Chemistry, University of Granada, 18071 Granada, Spain
Interests: synthesis; organic chemistry; natural products
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The synthesis of natural products is an important application of organic chemistry that has contributed to the development of new synthetic methods and strategies for the preparation and study of the structure as well as reactivity of complex natural products and their derivatives, especially those with high biological activity. The origin of this application could be related to structural elucidation studies, when modern physical and spectroscopic methods were not available, using degradation reactions and the partial synthesis of fragments or, in some cases, the total synthesis of a natural product itself. In addition, these procedures also allow for the establishment of the absolute stereochemistry of optically active compounds.

On the other hand, interest in natural product synthesis has also been related to the fact that many types of important pharmaceutical compounds come from natural products, such as antibiotics and steroid hormones. In addition, other secondary metabolites that play a role in regulating cellular and other biological processes are an incentive for natural product synthesis and the development of small-molecule libraries, as well as ultimately drug candidates based on natural product leads. In this sense, it is important to note that the quantities of natural products available from natural sources are limited. Thus, total or semi-synthesis is required to provide sufficient amounts for further biological characterization, a necessary step to determine if a natural product warrants further exploration as a lead structure for drug development.

For these reasons, interest in the synthesis of natural products has stimulated incredible advances in the development of new synthetic methods and strategies for the synthesis of structurally and stereochemically diverse molecules.

In this Special Issue, we intend to collect original research articles, communications, and review papers that cover the latest news in this field, especially in the context of the development of new synthetic methodologies and approaches to the preparation of bioactive natural compounds.

Prof. Dr. José Justicia
Prof. Dr. Rachid Chahboun
Guest Editors

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.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • natural products
  • biological activity
  • organic synthesis
  • terpenes
  • alkaloids
  • structural diversity

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Published Papers (3 papers)

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Research

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12 pages, 3029 KiB  
Article
Palladium-Catalyzed Acetoxylation of γ-Dehydro-aryl-himachalene: The Synthesis of a Novel Allylic Acetoxylated Sesquiterpene and a π-Allyl Palladium(II) Complex
by Issam Louchachha, Abdelmajid Faris, Youssef Edder, Ali Hasnaoui, Anna Kozakiewicz-Piekarz, Abdelkarim Ait Mansour, Brahim Boualy, Rachid Salghi, Khalil Azzaoui, Rachid Sabbahi, Ashwag S. Alanazi, Mohamed Hefnawy, Belkheir Hammouti, Abdallah Karim and Mustapha Ait Ali
Molecules 2024, 29(21), 5040; https://doi.org/10.3390/molecules29215040 - 25 Oct 2024
Viewed by 1116
Abstract
Allylic oxygenated derivatives of himachalenes are highly valued molecules due to their potential applications in perfumery, cosmetics, and pharmaceuticals. Previous attempts at catalyzed allylic oxidation of himachalenes led to the formation of a very stable η3-allyl palladium complex, preventing any further [...] Read more.
Allylic oxygenated derivatives of himachalenes are highly valued molecules due to their potential applications in perfumery, cosmetics, and pharmaceuticals. Previous attempts at catalyzed allylic oxidation of himachalenes led to the formation of a very stable η3-allyl palladium complex, preventing any further reaction development. Herein, we present the first successful palladium-catalyzed synthesis of a novel allylic acetoxylated derivative of himachalenes. This reaction was achieved by incorporating an aromatic ring into the substrate structure. The resulting intermediate complex was isolated and characterized using nuclear magnetic resonance spectroscopy and X-ray crystallography. Density functional theory (DFT) calculations were performed to compare the reactivity of the newly synthesized complex with previously reported ones. The theoretical results confirm that the introduction of an aromatic ring enhances the reactivity of the η³-allyl palladium complex, thereby facilitating the desired transformation. Full article
(This article belongs to the Special Issue Recent Advances in the Organic Synthesis of Bioactive Compounds)
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24 pages, 3145 KiB  
Article
Cheminformatics-Guided Exploration of Synthetic Marine Natural Product-Inspired Brominated Indole-3-Glyoxylamides and Their Potentials for Drug Discovery
by Darren C. Holland, Dale W. Prebble, Mark J. Calcott, Wayne A. Schroder, Francesca Ferretti, Aaron Lock, Vicky M. Avery, Milton J. Kiefel and Anthony R. Carroll
Molecules 2024, 29(15), 3648; https://doi.org/10.3390/molecules29153648 - 1 Aug 2024
Viewed by 2407
Abstract
Marine natural products (MNPs) continue to be tested primarily in cellular toxicity assays, both mammalian and microbial, despite most being inactive at concentrations relevant to drug discovery. These MNPs become missed opportunities and represent a wasteful use of precious bioresources. The use of [...] Read more.
Marine natural products (MNPs) continue to be tested primarily in cellular toxicity assays, both mammalian and microbial, despite most being inactive at concentrations relevant to drug discovery. These MNPs become missed opportunities and represent a wasteful use of precious bioresources. The use of cheminformatics aligned with published bioactivity data can provide insights to direct the choice of bioassays for the evaluation of new MNPs. Cheminformatics analysis of MNPs found in MarinLit (n = 39,730) up to the end of 2023 highlighted indol-3-yl-glyoxylamides (IGAs, n = 24) as a group of MNPs with no reported bioactivities. However, a recent review of synthetic IGAs highlighted these scaffolds as privileged structures with several compounds under clinical evaluation. Herein, we report the synthesis of a library of 32 MNP-inspired brominated IGAs (25–56) using a simple one-pot, multistep method affording access to these diverse chemical scaffolds. Directed by a meta-analysis of the biological activities reported for marine indole alkaloids (MIAs) and synthetic IGAs, the brominated IGAs 25–56 were examined for their potential bioactivities against the Parkinson’s Disease amyloid protein alpha synuclein (α-syn), antiplasmodial activities against chloroquine-resistant (3D7) and sensitive (Dd2) parasite strains of Plasmodium falciparum, and inhibition of mammalian (chymotrypsin and elastase) and viral (SARS-CoV-2 3CLpro) proteases. All of the synthetic IGAs tested exhibited binding affinity to the amyloid protein α-syn, while some showed inhibitory activities against P. falciparum, and the proteases, SARS-CoV-2 3CLpro, and chymotrypsin. The cellular safety of the IGAs was examined against cancerous and non-cancerous human cell lines, with all of the compounds tested inactive, thereby validating cheminformatics and meta-analyses results. The findings presented herein expand our knowledge of marine IGA bioactive chemical space and advocate expanding the scope of biological assays routinely used to investigate NP bioactivities, specifically those more suitable for non-toxic compounds. By integrating cheminformatics tools and functional assays into NP biological testing workflows, we can aim to enhance the potential of NPs and their scaffolds for future drug discovery and development. Full article
(This article belongs to the Special Issue Recent Advances in the Organic Synthesis of Bioactive Compounds)
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Review

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18 pages, 3204 KiB  
Review
Progress on the Synthesis of the Aromathecin Family of Compounds: An Overview
by Takashi Nishiyama, Shota Mizuno, Yuhzo Hieda and Tominari Choshi
Molecules 2024, 29(10), 2380; https://doi.org/10.3390/molecules29102380 - 18 May 2024
Viewed by 1125
Abstract
We present a systematic review of the methods developed for the synthesis of the aromathecin family of compounds (benz[6,7]indolizino[1,2-b]quinolin-11(13H)-ones) and their derivatives. These methods can be broadly classified into four categories based on the construction of pentacyclic structures: Category [...] Read more.
We present a systematic review of the methods developed for the synthesis of the aromathecin family of compounds (benz[6,7]indolizino[1,2-b]quinolin-11(13H)-ones) and their derivatives. These methods can be broadly classified into four categories based on the construction of pentacyclic structures: Category 1: by constructing a pyridone moiety (D-ring) on the pyrroloquinoline ring (A/B/C-ring), Category 2: by constructing a pyridine moiety (B-ring) on the pyrroloisoquinolone ring (C/D/E-ring), Category 3: by constructing an indolizidinone moiety (C/D-ring) in a tandem reaction, and Category 4: by constructing a pyrrolidine moiety (C-ring) on the isoquinolone ring (D/E-ring). Full article
(This article belongs to the Special Issue Recent Advances in the Organic Synthesis of Bioactive Compounds)
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