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Heterocyclic Chemistry with Applications (Second Edition)
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Heterocyclic Chemistry with Applications (Second Edition)

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

Deadline for manuscript submissions: 30 June 2025 | Viewed by 3900

Special Issue Editors

Dr. Hachemi Kadri

E-Mail Website
Guest Editor
Department of Pharmacy, School of Life Sciences, Pharmacy & Chemistry, Kingston University, Penrhyn Road, Kingston upon Thames KT1 2EE, UK
Interests: medicinal and pharmaceutical chemistry; drug discovery; biopharmaceuticals
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Fawaz Aldabbagh

E-Mail Website
Guest Editor
Department of Pharmacy, School of Life Sciences, Pharmacy & Chemistry, Kingston University, Penrhyn Road, Kingston upon Thames KT1 2EE, UK
Interests: free radical organic and polymer chemistry; heterocyclic and medicinal chemistry
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

This Special Issue, now in its second edition, focuses on the diverse applications of heterocycles, particularly in materials science and medicine. Heterocycles typically consist of five or six-membered rings, which may be fused or standalone, and often contain nitrogen and/or oxygen atoms. Due to their versatile structures, heterocycles are essential in multiple fields, including medicinal chemistry for antibiotics and anticancer drugs, agriculture for pesticides, materials science for organic electronics, and catalysis for key reactions. They also aid in environmental applications for pollutant degradation and support green chemistry, making them indispensable in research and industry. We eagerly anticipate receiving research articles, communications, and reviews that present the latest developments in heterocyclic chemistry, with applications spanning medicinal, polymer, and synthetic chemistry, among other fields. The goal is to provide a comprehensive overview of current trends and future directions in the dynamic field of heterocyclic applications.

Dr. Hachemi Kadri
Prof. Dr. Fawaz Aldabbagh
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

  • heterocycles
  • medicinal chemistry
  • natural products
  • organic synthesis
  • synthetic methods
  • drug discovery
  • nucleosides
  • biologically active heterocycles

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Related Special Issue

Published Papers (4 papers)

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Research

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12 pages, 3217 KiB  
Article
Decarboxylation-Driven Double Annulations: Innovative Multi-Component Reaction Pathways
by Desheng Zhan, Gang Yang, Tieli Zhou, Sashirekha Nallapati and Xiaofeng Zhang
Molecules 2025, 30(7), 1594; https://doi.org/10.3390/molecules30071594 - 2 Apr 2025
Viewed by 157
Abstract
A concerted five-component reaction strategy has been developed, featuring double [3+2] cycloadditions utilizing aspartic acid. This approach provides valuable insights into mechanistic pathways, allowing for the distinction between concerted and stepwise processes based on reaction efficiency and diastereoselectivity. Both aspartic and glutamic acids [...] Read more.
A concerted five-component reaction strategy has been developed, featuring double [3+2] cycloadditions utilizing aspartic acid. This approach provides valuable insights into mechanistic pathways, allowing for the distinction between concerted and stepwise processes based on reaction efficiency and diastereoselectivity. Both aspartic and glutamic acids have been employed for a thorough evaluation and exploration of decarboxylation-driven double annulations. This method effectively constructs pyrrolizidine frameworks through a concerted double 1,3-dipolar cycloaddition with aspartic acid, as well as tetrahydropyrrolizinones via three-component double annulations, which include decarboxylative 1,3-dipolar cycloaddition and lactamization with glutamic acid. These highly convergent, decarboxylation-driven multicomponent reactions (MCRs) efficiently produce fused polyheterocyclic systems while being environmentally friendly, generating only CO2 and water as byproducts. Full article
(This article belongs to the Special Issue Heterocyclic Chemistry with Applications (Second Edition))
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13 pages, 3256 KiB  
Article
Heteroaryl-Fused Triazapentalenes: Synthesis and Aggregation-Induced Emission
by Yingchun Wang, Thanh Chung Pham, Jianjun Huang, Junfeng Wu and Wim Dehaen
Molecules 2025, 30(1), 156; https://doi.org/10.3390/molecules30010156 - 3 Jan 2025
Viewed by 793
Abstract
A pyridine-fused triazapentalene shows weak fluorescence in solution and is readily accessible via nitrene-mediated cyclization. In this study, a modified Cadogan reaction was used to synthesize HetATAP 1. Palladium-catalyzed reactions have been used as post-functionalization methods. Interestingly, modified Suzuki cross-couplings with various [...] Read more.
A pyridine-fused triazapentalene shows weak fluorescence in solution and is readily accessible via nitrene-mediated cyclization. In this study, a modified Cadogan reaction was used to synthesize HetATAP 1. Palladium-catalyzed reactions have been used as post-functionalization methods. Interestingly, modified Suzuki cross-couplings with various boronic acids resulted in poor to moderate yields of HetATAPs 2–5 which were arylated at the azole moiety. Direct CH arylation of HetATAP 1 gave the products with the same regiochemistry in satisfactory yields. The structures of HetATAPs 2–5 were confirmed using NMR analysis. In addition, the photophysical properties of HetATAPs 1–5 were studied under various conditions. Particularly, the emission of HetATAPs 2–5 is enhanced in the solid and aggregate state. Full article
(This article belongs to the Special Issue Heterocyclic Chemistry with Applications (Second Edition))
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12 pages, 2022 KiB  
Article
Synthesis of New Isoxazolidine Derivatives Utilizing the Functionality of N-Carbonylpyrazol-Linked Isoxazolidines
by Xixian Cao, Jun You, Yunze Wang, Yanchao Yu, Wenju Wu and Yifang Liang
Molecules 2024, 29(15), 3454; https://doi.org/10.3390/molecules29153454 - 23 Jul 2024
Viewed by 1149
Abstract
Using Ni(II) as the catalyst, electron-deficient 3,5-dimethylacryloylpyrazole olefin was reacted with C,N-diarylnitrones alone for 10 min to prepare novel five-member heterocyclic products, 4-3,5-dimethylacryloylpyrazole isoxazolidines with 100% regioselectivity and up to 99% yield. And then, taking these cycloadducts as substrates, six [...] Read more.
Using Ni(II) as the catalyst, electron-deficient 3,5-dimethylacryloylpyrazole olefin was reacted with C,N-diarylnitrones alone for 10 min to prepare novel five-member heterocyclic products, 4-3,5-dimethylacryloylpyrazole isoxazolidines with 100% regioselectivity and up to 99% yield. And then, taking these cycloadducts as substrates, six kinds of derivatization reactions, like ring-opening, nucleophilic substitution, addition-elimination and reduction, were studied. Experimental results showed that all kinds of transformations could obtain the target products at a high conversion rate under mild conditions, a finding which provided the basic methods for organic synthesis methodology research based on an isoxazolidine skeleton. Full article
(This article belongs to the Special Issue Heterocyclic Chemistry with Applications (Second Edition))
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Review

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15 pages, 3623 KiB  
Review
Nucleoside Analogues for Chagas Disease and Leishmaniasis Therapy: Current Status and Future Perspectives
by Emmanuel Awucha Nwoke, Silvester Lowe, Fawaz Aldabbagh, Karunakaran Kalesh and Hachemi Kadri
Molecules 2024, 29(22), 5234; https://doi.org/10.3390/molecules29225234 - 5 Nov 2024
Viewed by 1267
Abstract
Chagas disease and leishmaniasis are two neglected tropical diseases that affect millions of people in low- and middle-income tropical countries. These diseases caused by protozoan parasites pose significant global health challenges, which have been exacerbated by the recent COVID-19 pandemic. There is an [...] Read more.
Chagas disease and leishmaniasis are two neglected tropical diseases that affect millions of people in low- and middle-income tropical countries. These diseases caused by protozoan parasites pose significant global health challenges, which have been exacerbated by the recent COVID-19 pandemic. There is an urgent need for novel therapeutics as current treatments are limited by toxicity and drug resistance. Nucleoside analogues, which have been extensively studied and successfully applied in antiviral and antitumor therapies, hold potential that has yet to be fully explored for treating these neglected diseases. In this review, we discuss the use of nucleoside analogues as promising therapeutic agents for Chagas disease and leishmaniasis. After briefly examining the pathology, progression, and current treatment options for these diseases, we provide a comprehensive analysis of the status of nucleoside analogues and explore their prospects. By outlining the current landscape and future directions, this review aims to guide research and development efforts towards more effective nucleoside-based treatments for Chagas disease and leishmaniasis. Full article
(This article belongs to the Special Issue Heterocyclic Chemistry with Applications (Second Edition))
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