Special Issue "Heterocyclic Compounds and Their Application in Therapy"

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: 30 November 2021.

Special Issue Editors

Prof. Dr. Thierry Besson
E-Mail Website
Guest Editor
Normandie Univ, UNIROUEN, INSA Rouen, CNRS, COBRA UMR 6014, F-76000 Rouen, France
Interests: chemistry of heterocyclic compounds; microwave-assisted chemistry; kinase inhibitors; green chemistry applied to bioactive compounds; Alzheimer's disease; Down syndrome; cancer
Special Issues and Collections in MDPI journals
Prof. Dr. Pascal Marchand
E-Mail Website
Guest Editor
Université de Nantes, Cibles et médicaments des infections et du cancer, IICiMed, EA 1155, F-44000 Nantes, France
Interests: design; synthesis and biological evaluation of heterocyclic compounds for therapeutic purposes (mycology, parasitology, and cancer); inhibitors of kinase signaling pathways; ADMET properties of molecules of biological interest
Special Issues and Collections in MDPI journals

Special Issue Information

Dear Colleagues,

Heterocycles are present in numerous organic compounds of interest in biology, pharmacology, and medicine. Aromatic and non-aromatic molecules are still one of the largest areas of research in organic and medicinal chemistry. Exploring novel techniques or methods for synthesizing and functionalizing these compounds has been boosted, until becoming one of the major axes of sustainable chemistry. Heterocycles exhibit unique structures leading to several applications in the design of drugs. Presence of heteroatoms (e.g., N, S, and O) in the cyclic molecular structures results in significant physicochemical properties. Hydrogen-bond donors and acceptors in these rigid frameworks allow hydrogen-bond interactions with receptors and/or target enzymes, enhancing binding affinity and improving therapeutic potency. Heterocycles can also be involved in the design of prodrugs and can modulate the lipophilicity of bioactive molecules, thus varying their pharmacokinetic and pharmaceutical properties. This Special Issue aims to review recent developments in the design, synthesis, and pharmaceutical properties of natural products and synthetic compounds containing aromatic heterocyclic systems. 

Prof. Dr. Thierry Besson
Prof. Dr. Pascal Marchand
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 papers will be 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. Pharmaceuticals is an international peer-reviewed open access monthly 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 1800 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

  • medicinal chemistry
  • bioactive heterocyclic compounds
  • chemical space
  • chemical tools
  • innovative and sustainable synthetic routes
  • molecular modelling studies
  • pharmacological properties
  • prodrugs: design and development
  • in vitro and in vivo studies

Published Papers (2 papers)

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Research

Open AccessArticle
Design, Synthesis, and Antibacterial Screening of Some Novel Heteroaryl-Based Ciprofloxacin Derivatives as DNA Gyrase and Topoisomerase IV Inhibitors
Pharmaceuticals 2021, 14(5), 399; https://0-doi-org.brum.beds.ac.uk/10.3390/ph14050399 - 22 Apr 2021
Viewed by 289
Abstract
A novel series of ciprofloxacin hybrids comprising various heterocycle derivatives has been synthesized and structurally elucidated using 1H NMR, 13C NMR, and elementary analyses. Using ciprofloxacin as a reference, compounds 121 were screened in vitro against Gram-positive bacterial strains [...] Read more.
A novel series of ciprofloxacin hybrids comprising various heterocycle derivatives has been synthesized and structurally elucidated using 1H NMR, 13C NMR, and elementary analyses. Using ciprofloxacin as a reference, compounds 121 were screened in vitro against Gram-positive bacterial strains such as Staphylococcus aureus and Bacillus subtilis and Gram-negative strains such as Escherichia coli and Pseudomonas aeruginosa. As a result, many of the compounds examined had antibacterial activity equivalent to ciprofloxacin against test bacteria. Compounds 26, oxadiazole derivatives, were found to have antibacterial activity that was 88 to 120% that of ciprofloxacin against Gram-positive and Gram-negative bacteria. The findings showed that none of the compounds tested had antifungal activity against Aspergillus flavus, but did have poor activity against Candida albicans, ranging from 23% to 33% of fluconazole, with compound 3 being the most active (33% of fluconazole). The most potent compounds, 3, 4, 5, and 6, displayed an IC50 of 86, 42, 92, and 180 nM against E. coli DNA gyrase, respectively (novobiocin, IC50 = 170 nM). Compounds 4, 5, and 6 showed IC50 values (1.47, 6.80, and 8.92 µM, respectively) against E. coli topo IV in comparison to novobiocin (IC50 = 11 µM). Full article
(This article belongs to the Special Issue Heterocyclic Compounds and Their Application in Therapy)
Open AccessArticle
Novel Potent and Selective DPP-4 Inhibitors: Design, Synthesis and Molecular Docking Study of Dihydropyrimidine Phthalimide Hybrids
Pharmaceuticals 2021, 14(2), 144; https://0-doi-org.brum.beds.ac.uk/10.3390/ph14020144 - 11 Feb 2021
Viewed by 451
Abstract
Background: Dipeptidyl peptidase-4 (DPP-4) inhibitors have emerged as anti-hyperglycemic agents that improve glycemic control in type 2 diabetic patients, either as monotherapy or in combination with other antidiabetic drugs. Methods: A novel series of dihydropyrimidine phthalimide hybrids was synthesized and evaluated for their [...] Read more.
Background: Dipeptidyl peptidase-4 (DPP-4) inhibitors have emerged as anti-hyperglycemic agents that improve glycemic control in type 2 diabetic patients, either as monotherapy or in combination with other antidiabetic drugs. Methods: A novel series of dihydropyrimidine phthalimide hybrids was synthesized and evaluated for their in vitro and in vivo DPP-4 inhibition activity and selectivity using alogliptin as reference. Oral glucose tolerance test was assessed in type 2 diabetic rats after chronic treatment with the synthesized hybrids ± metformin. Cytotoxicity and antioxidant assays were performed. Additionally, molecular docking study with DPP-4 and structure activity relationship of the novel hybrids were also studied. Results: Among the synthesized hybrids, 10g, 10i, 10e, 10d and 10b had stronger in vitro DPP-4 inhibitory activity than alogliptin. Moreover, an in vivo DPP-4 inhibition assay revealed that 10g and 10i have the strongest and the most extended blood DPP-4 inhibitory activity compared to alogliptin. In type 2 diabetic rats, hybrids 10g, 10i and 10e exhibited better glycemic control than alogliptin, an effect that further supported by metformin combination. Finally, 10j, 10e, 10h and 10d had the highest radical scavenging activity in DPPH assay. Conclusions: Hybrids 10g, 10i and 10e are potent DPP-4 inhibitors which may be beneficial for T2DM treatment. Full article
(This article belongs to the Special Issue Heterocyclic Compounds and Their Application in Therapy)
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