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Synthesis and Biologically Relevant Heterocyclic Compounds
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Synthesis and Biologically Relevant Heterocyclic Compounds

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

Deadline for manuscript submissions: 31 July 2024 | Viewed by 3138

Special Issue Editor

Dr. Gheorghita Zbancioc

E-Mail Website1 Website2
Guest Editor
Chemistry Department, Alexandru Ioan Cuza University of Iasi, 700506 Iasi, Romania
Interests: diazines; medicinal chemistry; anticancer; antituberculosis; microwave; ultrasounds; organic synthesis
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Heterocyclic compounds are important privileged scaffolds in medicinal chemistry and drug discovery. These compounds are described to have a wide range of biological activities, including anti-bacterial, anti-cancer, anti-fungal, anti-viral, anti-plasmodial, anti-malarial, anti-inflammatory, anti-tubercular, anti-hypertensive, anti-thrombic, anti-coagulant, diuretic, and analgesic characteristics, among other things.

Two aggressive life-threatening diseases—cancer and tuberculosis—are being actively fought by the pharmaceutical industry and contemporary medicine. Millions of people die each year from these two diseases, which are the main causes of death worldwide. Their incidence is rising, and their treatments are becoming more sophisticated and complex. Because of the wide range of neoplasm kinds, high toxicity levels, the non-specificity of medications, the evolution of drug resistance, and multidrug resistance, cancer chemotherapy is complicated, expensive, and frequently fairly ineffective.

This Special Issue's purpose is to offer an opportunity for the latest research on the synthesis of biologically active heterocycle derivatives, including (but not limited to) those with anti-cancer, anti-tuberculosis, and anti-bacterial characteristics.

Dr. Gheorghita Zbancioc
Guest Editor

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
  • azines
  • azoles
  • anti-cancer
  • anti-tuberculosis
  • anti-microbial
  • medicinal chemistry

Published Papers (3 papers)

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Research

11 pages, 2363 KiB  
Article
Novel Derivatives of Nitrobenzofurazan with Chromogenic and Fluorogenic Properties
by Alexandru Bujor, Anamaria Hanganu, Rodica Baratoiu, Elena N. Hristea, Madalina Tudose, Victorita Tecuceanu, Augustin M. Madalan and Petre Ionita
Molecules 2023, 28(16), 6146; https://doi.org/10.3390/molecules28166146 - 20 Aug 2023
Viewed by 723
Abstract
Five new derivatives were obtained utilizing 4-chloro-7-nitrobenzofurazan (NBD-chloride) in combination with furfurylamine, adamantylamine, aminohippuric acid, phenylalanine, and dehydroabietylamine. These derivatives were then subjected to a comparative analysis of their physical, chemical, and certain biological properties alongside two analogous and known compounds derived from [...] Read more.
Five new derivatives were obtained utilizing 4-chloro-7-nitrobenzofurazan (NBD-chloride) in combination with furfurylamine, adamantylamine, aminohippuric acid, phenylalanine, and dehydroabietylamine. These derivatives were then subjected to a comparative analysis of their physical, chemical, and certain biological properties alongside two analogous and known compounds derived from the glycine and 4-amino-TEMPO free radical. Full article
(This article belongs to the Special Issue Synthesis and Biologically Relevant Heterocyclic Compounds)
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13 pages, 3474 KiB  
Article
The Amoebicidal Activity of Diferrocenyl Derivatives: A Significant Dependence on the Electronic Environment
by Yanis Toledano-Magaña, Mario Néquiz, Lucía Margarita Valenzuela-Salas, Jessica J. Sánchez-García, Rodrigo Galindo-Murillo, Juan Carlos García-Ramos and Elena I. Klimova
Molecules 2023, 28(16), 6008; https://doi.org/10.3390/molecules28166008 - 11 Aug 2023
Viewed by 795
Abstract
Amoebiasis is the second leading cause of death worldwide associated with parasitic disease and is becoming a critical health problem in low-income countries, urging new treatment alternatives. One of the most promising strategies is enhancing the redox imbalance within these susceptible parasites related [...] Read more.
Amoebiasis is the second leading cause of death worldwide associated with parasitic disease and is becoming a critical health problem in low-income countries, urging new treatment alternatives. One of the most promising strategies is enhancing the redox imbalance within these susceptible parasites related to their limited antioxidant defense system. Metal-based drugs represent a perfect option due to their extraordinary capacity to stabilize different oxidation states and adopt diverse geometries, allowing their interaction with several molecular targets. This work describes the amoebicidal activity of five 2-(Z-2,3-diferrocenylvinyl)-4X-4,5-dihydrooxazole derivatives (X = H (3a), Me (3b), iPr (3c), Ph (3d), and benzyl (3e)) on Entamoeba histolytica trophozoites and the physicochemical, experimental, and theoretical properties that can be used to describe the antiproliferative activity. The growth inhibition capacity of these organometallic compounds is strongly related to a fine balance between the compounds’ redox potential and hydrophilic character. The antiproliferative activity of diferrocenyl derivatives studied herein could be described either with the redox potential, the energy of electronic transitions, logP, or the calculated HOMO–LUMO values. Compound 3d presents the highest antiproliferative activity of the series with an IC50 of 23 µM. However, the results of this work provide a pipeline to improve the amoebicidal activity of these compounds through the directed modification of their electronic environment. Full article
(This article belongs to the Special Issue Synthesis and Biologically Relevant Heterocyclic Compounds)
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14 pages, 2709 KiB  
Article
Fused Triazinobenzimidazoles Bearing Heterocyclic Moiety: Synthesis, Structure Investigations, and In Silico and In Vitro Biological Activity
by Kameliya Anichina, Nikolai Georgiev, Nikolay Lumov, Dimitar Vuchev, Galya Popova-Daskalova, Georgi Momekov, Emiliya Cherneva, Rositsa Mihaylova, Anelia Mavrova, Stela Atanasova-Vladimirova, Iskra Piroeva and Denitsa Yancheva
Molecules 2023, 28(13), 5034; https://doi.org/10.3390/molecules28135034 - 27 Jun 2023
Cited by 2 | Viewed by 1333
Abstract
[1,3,5]Triazino[1,2-a]benzimidazole-2-amines bearing heterocyclic moiety in 4-position were synthesized. The compounds were characterized by elemental analysis, IR, 1H-NMR, 13C-NMR, and HRMS spectroscopy. The molecular geometry and electron structure of these molecules were theoretically studied using density functional theory (DFT) methods. [...] Read more.
[1,3,5]Triazino[1,2-a]benzimidazole-2-amines bearing heterocyclic moiety in 4-position were synthesized. The compounds were characterized by elemental analysis, IR, 1H-NMR, 13C-NMR, and HRMS spectroscopy. The molecular geometry and electron structure of these molecules were theoretically studied using density functional theory (DFT) methods. The molecular structure of the synthesized fused triazinobenzimidazole was confirmed to correspond to the 3,4-dihydrotriazinobenzimidazole structure through the analysis of spectroscopic NMR data and DFT calculations. The antinematodic activity was evaluated in vitro on isolated encapsulated muscle larvae (ML) of Trichinella spiralis. The results showed that the tested triazinobenzimidazoles exhibit significantly higher efficiency than the conventional drug used to treat trichinosis, albendazole, at a concentration of 50 μg/mL. The compound 3c substituted with a thiophen-2-yl moiety exhibited the highest anthelmintic activity, with a larvicidal effect of 58.41% at a concentration of 50 μg/mL after 24 h of incubation. Following closely behind, the pyrrole analog 3f demonstrated 49.90% effectiveness at the same concentration. The preliminary structure-anti-T. spiralis activity relationship (SAR) of the analogues in the series was discussed. The cytotoxicity of the benzimidazole derivatives against two normal fibroblast cells (3T3 and CCL-1) and two cancer human cell lines (MCF-7 breast cancer cells and chronic myeloid leukemia cells AR-230) was evaluated using the MTT-dye reduction assay. The screening results indicated that the compounds showed no cytotoxicity against the tested cell lines. An in silico study of the physicochemical and pharmacokinetic characteristics of the novel synthesized fused triazinobenzimidazoles showed that they were characterized by a significant degree of drug-likeness and optimal properties for anthelmintic agents. Full article
(This article belongs to the Special Issue Synthesis and Biologically Relevant Heterocyclic Compounds)
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