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Heterocyclic Compounds: Discovery, Synthesis and Applications

A special issue of Applied Sciences (ISSN 2076-3417). This special issue belongs to the section "Applied Biosciences and Bioengineering".

Deadline for manuscript submissions: 20 July 2026 | Viewed by 3208

Special Issue Editor


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Guest Editor
1. Department of Science, University of Basilicata, Viale dell’Ateneo Lucano 10, 85100 Potenza, Italy
2. Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Arcavacata di Rende, Italy
Interests: carbazole derivatives; heterocyclic compounds synthesis; antioxidants; medicinal chemistry; medicinal compounds synthesis
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Special Issue Information

Dear Colleagues,

Heterocyclic compounds containing sulphur, oxygen or nitrogen have attracted particular interest among researchers. Many biologically active agents, both of natural and synthetic origin, bear a heterocyclic structure (for example, ellipticine, papaverine, emetine, theophylline, atropine, codeine, reserpine, morphine, diazepam, chlorpromazine, amiodarone, bergapten and barbiturates). These compounds represent a great concern due to the attractive structural characteristics and encouraging therapeutic effects, including antitumor, antiviral, antibacterial, antimicrobial, antifungal, anti-inflammatory, pain-relieving, anxiolytic and antihistamine activity. Thus, several heterocyclic compounds possess various industrial applications, and they are used in pharmaceutical, dyes, insecticides and plastic industries. This Special Issue will publish research papers with topics including, but not limited to, the synthesis and/or application of heterocycles endowed with any biological action. We also welcome contributions that highlight the importance of the sulphur, oxygen or nitrogen-based scaffolds that are widely found in cosmetics, dyes, agrochemicals and functional materials. Therefore, in this Special Issue, we will accept research papers and review articles addressing studies on the molecular modelling, synthesis, delivery systems, biological, nutritional, phytochemical evaluation and all applications of heterocycle compounds.

Dr. Anna Caruso
Guest Editor

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Keywords

  • heterocyclic compounds
  • N-containing heterocycle
  • O-containing heterocycle
  • S-containing heterocycle
  • medicinal chemistry
  • drug development
  • industrial applications
  • therapeutic agent
  • biological activity

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Published Papers (2 papers)

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Research

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20 pages, 666 KB  
Article
Synthesis and Antibacterial Evaluation of 5-Aminosalicylic Acid Derivatives
by Kazimieras Anusevičius, Jūratė Šiugždaitė, Birutė Sapijanskaitė-Banevič, Valentas Špiliauskas, Birutė Grybaitė, Livija Tubytė and Vytautas Mickevičius
Appl. Sci. 2026, 16(2), 703; https://doi.org/10.3390/app16020703 - 9 Jan 2026
Viewed by 575
Abstract
The anti-inflammatory scaffold 5-aminosalicylic acid, which is widely used in therapeutic applications, was chosen for the synthesis of N-[3-(hydrazinecarbonyl)-4-hydroxyphenyl]acetamide (1) to enhance its antibacterial properties. The condensation of hydrazide 1 with aromatic aldehydes provided hydrazone derivatives 2af, [...] Read more.
The anti-inflammatory scaffold 5-aminosalicylic acid, which is widely used in therapeutic applications, was chosen for the synthesis of N-[3-(hydrazinecarbonyl)-4-hydroxyphenyl]acetamide (1) to enhance its antibacterial properties. The condensation of hydrazide 1 with aromatic aldehydes provided hydrazone derivatives 2af, whereas cyclocondensation reactions and other related transformations afforded five-membered heterocycles, including pyrrole 3, pyrazole 4, pyrrolidinone 7, oxadiazoles 9, 10, thiadiazole 14, and triazole 15. Additional modifications yielded acetylhydrazine derivative 11, which was O-alkylated to analogue 12. Antibacterial evaluation showed stronger activity against Gram-positive bacteria such as S. aureus and MRSA than against Gram-negative strains of E. coli and S. Enteritidis, consistent with differences in cell membrane permeability. Notably, derivatives containing pyrrolidinone 7, thiosemicarbazide 13, and 1,3,4-thiadiazole 14 exhibited potent bactericidal activity against S. aureus and MRSA, while hydrazones 2b, 2c, 2f, pyrrole 3, and pyrrolidinone 7 exhibited activity against E. coli. These results provide a practical strategy for the discovery of heterocyclic compounds and emphasise the potential of functionalised 5-aminosalicylic acid derivatives as prime candidates for the development of broad-spectrum antibacterial agents. Full article
(This article belongs to the Special Issue Heterocyclic Compounds: Discovery, Synthesis and Applications)
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Review

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15 pages, 1486 KB  
Review
The Potential of Indole Alkaloids in Bone Health and Osteoporosis Management
by Anna Caruso, Virginia Caira, Hussein El-Kashef and Carmela Saturnino
Appl. Sci. 2024, 14(18), 8124; https://doi.org/10.3390/app14188124 - 10 Sep 2024
Cited by 5 | Viewed by 1923
Abstract
Indole alkaloids, a class of plant-derived nitrogen-containing compounds, have emerged as promising candidates for osteoporosis treatment. Their favorable biocompatibility profile demonstrated efficacy in preclinical models, and low reported toxicity make them attractive alternatives to existing therapies. This review focuses on the therapeutic potential [...] Read more.
Indole alkaloids, a class of plant-derived nitrogen-containing compounds, have emerged as promising candidates for osteoporosis treatment. Their favorable biocompatibility profile demonstrated efficacy in preclinical models, and low reported toxicity make them attractive alternatives to existing therapies. This review focuses on the therapeutic potential of specific indole alkaloids, including vindoline, rutaecarpine, harmine, and its derivatives, in promoting bone health and managing osteoporosis. Full article
(This article belongs to the Special Issue Heterocyclic Compounds: Discovery, Synthesis and Applications)
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