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Organic Synthesis in Natural Products and Bioactive Compounds

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

Deadline for manuscript submissions: closed (31 December 2022) | Viewed by 13055

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Prof. Dr. Florenci V. González

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Departament de química inorgànica i orgànica, Universitat Jaume I, Castelló, Spain
Interests: medicinal chemistry; organic synthesis; drug discovery; chemical probes; protease inhibitors
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Special Issue Information

Dear Colleagues,

Organic synthesis, the art and science of constructing substances, natural or designed, is the topic of this issue. Since Wöhler’s synthesis of urea in 1828, organic synthetic chemists have been able to replicate most intriguing natural products. New chemical reactions have been discovered expanding the methods in chemical synthesis and incorporating more tools to the synthetic toolbox: catalytic processes using metal catalysts and organocatalysts, umpolung reactions, new chemical reagents permitting to carry out known reactions under new conditions, and more.

Organic synthesis is the tool for the preparation of small molecules with interesting biological and medicinal properties—new compounds with activity against diseases affecting humankind today such as cancer, metabolic disorders, neurodegenerative disorders or infectious diseases, as well as new syntheses of known drugs. New bioactive compounds are designed and synthesized to target key metabolic reactions in pathological processes as the first steps toward drug discovery. The crosstalk between synthetic and medicinal chemists enable a high impact of new synthetic methodologies in drug discovery.

This Special Issue is dedicated to communications in the form of original research and review articles, which cover the total synthesis of natural products, synthetic methodology, and the design, synthesis, and activity of small molecules having biomedical properties. Review articles could discuss new synthetic approaches to a family of natural products, to a certain synthetic methodology, or to a group of drugs or bioactive compounds. If within the scope of organic synthesis, other types of molecules can also be considered for this Special Issue. Authors considering the submission of a review are kindly asked to provide in advance to the guest editor a brief outline of the subject matter of their work.

Prof. Dr. Florenci V. González
Guest Editor

Manuscript Submission Information

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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

Synthetic methodology
Biomedicinally active compounds
Total synthesis
Drugs synthesis

Published Papers (5 papers)

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Research

15 pages, 3784 KiB

Open AccessArticle

Identifying Terpenoid Biosynthesis Genes in Euphorbia maculata via Full-Length cDNA Sequencing

by Mi Jin Jeon, Neha Samir Roy, Beom-Soon Choi, Ji Yeon Oh, Yong-In Kim, Hye Yoon Park, Taeyoung Um, Nam-Soo Kim, Soonok Kim and Ik-Young Choi

Molecules 2022, 27(14), 4591; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules27144591 - 19 Jul 2022

Cited by 4 | Viewed by 1631

Abstract

The annual herb Euphorbia maculata L. produces anti-inflammatory and biologically active substances such as triterpenoids, tannins, and polyphenols, and it is used in traditional Chinese medicine. Of these bioactive compounds, terpenoids, also called isoprenoids, are major secondary metabolites in E. maculata. Full-length cDNA sequencing was carried out to characterize the transcripts of terpenoid biosynthesis reference genes and determine the copy numbers of their isoforms using PacBio SMRT sequencing technology. The Illumina short-read sequencing platform was also employed to identify differentially expressed genes (DEGs) in the secondary metabolite pathways from leaves, roots, and stems. PacBio generated 62 million polymerase reads, resulting in 81,433 high-quality reads. From these high-quality reads, we reconstructed a genome of 20,722 genes, in which 20,246 genes (97.8%) did not have paralogs. About 33% of the identified genes had two or more isoforms. DEG analysis revealed that the expression level differed among gene paralogs in the leaf, stem, and root. Whole sets of paralogs and isoforms were identified in the mevalonic acid (MVA), methylerythritol phosphate (MEP), and terpenoid biosynthesis pathways in the E. maculata L. The nucleotide information will be useful for identifying orthologous genes in other terpenoid-producing medicinal plants. Full article

(This article belongs to the Special Issue Organic Synthesis in Natural Products and Bioactive Compounds)

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20 pages, 3704 KiB

Open AccessArticle

Synthesis of Polycyclic Ether-Benzopyrans and In Vitro Inhibitory Activity against Leishmania tarentolae

by Sarita Singh, Jacob P. Grabowski, Shilpa Pohani, C. Fiore Apuzzo, David C. Platt, Marjorie A. Jones and T. Andrew Mitchell

Molecules 2020, 25(22), 5461; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules25225461 - 21 Nov 2020

Cited by 2 | Viewed by 2053

Abstract

Construction of a focused library of polycyclic ether-benzopyrans was undertaken in order to discover new therapeutic compounds that affect Leishmania growth and infectivity. This is especially of interest since there are few drug therapies for leishmaniasis that do not have serious drawbacks such high cost, side effects, and emerging drug resistance. The construction of these polycyclic ether-benzopyrans utilized an acetoxypyranone-alkene [5+2] cycloaddition and the Suzuki-Miyaura cross-coupling. The multi-gram quantity of the requisite aryl bromide was obtained followed by effective Pd-catalyzed coupling with boronic acid derivatives. Compounds were tested in vitro using the parasitic protozoan, Leishmania tarentolae. Effects of concentration, time, and exposure to light were evaluated. In addition, the effects on secreted acid phosphatase activity and nitric oxide production were investigated, since both have been implicated in parasite infectivity. The data presented herein are indicative of disruption of the Leishmania tarentolae and thus provide impetus for the development and testing of a more extensive library. Full article

(This article belongs to the Special Issue Organic Synthesis in Natural Products and Bioactive Compounds)

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16 pages, 3046 KiB

Open AccessArticle

Tert-butyl-(4-hydroxy-3-((3-(2-methylpiperidin-yl)propyl)carbamoyl)phenyl)carbamate Has Moderated Protective Activity in Astrocytes Stimulated with Amyloid Beta 1-42 and in a Scopolamine Model

by Raúl Horacio Camarillo-López, Maricarmen Hernández Rodríguez, Mónica Adriana Torres-Ramos, Ivonne Maciel Arciniega-Martínez, Iohanan Daniel García-Marín, José Correa Basurto, Juan Vicente Méndez Méndez and Martha Cecilia Rosales-Hernández

Molecules 2020, 25(21), 5009; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules25215009 - 29 Oct 2020

Cited by 1 | Viewed by 2021

Abstract

Alzheimer’s disease (AD) is a neurodegenerative disease with no cure nowadays; there is no treatment either to prevent or to stop its progression. In vitro studies suggested that tert-butyl-(4-hydroxy-3-((3-(2-methylpiperidin-yl)propyl)carbamoyl)phenyl) carbamate named the M4 compound can act as both β-secretase and an acetylcholinesterase inhibitor, preventing the amyloid beta peptide (Aβ) aggregation and the formation of fibrils (fAβ) from Aβ_1-42. This work first aimed to assess in in vitro studies to see whether the death of astrocyte cells promoted by Aβ_1-42 could be prevented. Second, our work investigated the ability of the M4 compound to inhibit amyloidogenesis using an in vivo model after scopolamine administration. The results showed that M4 possesses a moderate protective effect in astrocytes against Aβ_1-42 due to a reduction in the TNF-α and free radicals observed in cell cultures. In the in vivo studies, however, no significant effect of M4 was observed in comparison with a galantamine model employed in rats, in which case this outcome was attributed to the bioavailability of M4 in the brain of the rats. Full article

(This article belongs to the Special Issue Organic Synthesis in Natural Products and Bioactive Compounds)

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16 pages, 5270 KiB

Open AccessArticle

Synthesis of a New Class of Spirooxindole–Benzo[b]Thiophene-Based Molecules as Acetylcholinesterase Inhibitors

by Assem Barakat, Saeed Alshahrani, Abdullah Mohammed Al-Majid, M. Ali, Mezna Saleh Altowyan, Mohammad Shahidul Islam, Abdullah Saleh Alamary, Sajda Ashraf and Zaheer Ul-Haq

Molecules 2020, 25(20), 4671; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules25204671 - 13 Oct 2020

Cited by 16 | Viewed by 2553

Abstract

A series of new oxindole-based spiro-heterocycles bearing the benzo[b]thiophene motif were synthesized via a 1,3-dipolar cycloaddition reaction and their acetylcholinesterase (AChE) inhibitory activity was evaluated. All the synthesized compounds exhibited moderate inhibitory activities against AChE, while IIc was found to be the most active analog with an IC₅₀ value of 20,840 µM·L⁻¹. Its molecular structure was a 5-chloro-substituted oxindole bearing benzo[b]thiophene and octahydroindole moieties. Based on molecular docking studies, IIc was strongly bound to the catalytic and peripheral anionic sites of the protein through hydrophilic, hydrophobic, and π-stacking interactions with Asp74, Trp86, Tyr124, Ser125, Glu202, Ser203, Trp236, Trp286, Phe297, Tyr337, and Tyr341. These interactions also indicated that the multiplicity of the IIc aromatic core significantly favored its activity. Full article

(This article belongs to the Special Issue Organic Synthesis in Natural Products and Bioactive Compounds)

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16 pages, 7039 KiB

Open AccessArticle

One Pot Synthesis of Micromolar BACE-1 Inhibitors Based on the Dihydropyrimidinone Scaffold and Their Thia and Imino Analogues

by Jessica Bais, Fabio Benedetti, Federico Berti, Iole Cerminara, Sara Drioli, Maria Funicello, Giorgia Regini, Mattia Vidali and Fulvia Felluga

Molecules 2020, 25(18), 4152; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules25184152 - 10 Sep 2020

Cited by 13 | Viewed by 3428

Abstract

A library of dihydropyrimidinones was synthesized via a “one-pot” three component Biginelli reaction using different aldehydes in combination with β-dicarbonyl compounds and urea. Selected 2-thiooxo and 2-imino analogs were also obtained with the Biginelli reaction from thiourea and guanidine hydrochloride, respectively. The products were screened in vitro for their β-secretase inhibitory activity. The majority of the compounds resulted to be active, with IC₅₀ in the range 100 nM–50 μM. Full article

(This article belongs to the Special Issue Organic Synthesis in Natural Products and Bioactive Compounds)

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