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Applied Sciences
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Heterocyclic Compounds with Potential Biological Activity - Volume II
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Heterocyclic Compounds with Potential Biological Activity - Volume II

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

Deadline for manuscript submissions: closed (20 September 2022) | Viewed by 17429

Special Issue Editor

Prof. Dr. Mariusz Mojzych

E-Mail Website1 Website2
Guest Editor
Department of Chemistry, Siedlce University of Natural Sciences and Humanities, 08-110 Siedlce, Poland
Interests: medicinal chemistry; medicinal and pharmaceutical chemistry; synthetic organic chemistry; heterocyclic chemistry
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The fact that heterocyclic compounds play particularly important functions in living organisms and have found many practical applications makes this group of derivatives a continuously interesting material for further research and new publications. They constitute a structural element of nucleic acids, i.e., chemical substances that carry the genetic information controlling inheritance. Some of the naturally occurring products, e.g., pigments, vitamins, alkaloids, and antibiotics, possess a heterocyclic core. Modern society is dependent on synthetic heterocycles that are predominantly used as pharmaceuticals, agrochemicals, and veterinary products. They also find applications as sanitizers, antioxidants, copolymers, dyes, and plastics. They are used as vehicles in the synthesis of other organic compounds. Due to the variety of modern methods for synthesis, the chemistry of heterocyclic compounds has recently developed rapidly and dynamically. This is evidenced in the growing trend toward the design and synthesis of a very large number of new heterocycles.

The aim of this Special Issue is to spot recent advances in “Heterocyclic Compounds with Potential Biological Activity”, including original research papers or up-to-date, comprehensive reviews, highlighting the recent identification of synthetic and natural molecules with potential biological activity and possible applications.

We believe that this Special Issue is a relevant and timely one, and we look forward to receiving your contributions.

Prof. Dr. Mariusz Mojzych
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. Applied Sciences 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 2400 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

  • heterocyclic compounds
  • drug discovery and synthesis
  • design and synthesis
  • bioactive compounds
  • total synthesis of natural products
  • modern methods synthesis
  • theoretical evaluation
  • in silico drug design
  • fused heterocycles
  • reactivity of heterocyclic compounds

Published Papers (5 papers)

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Research

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11 pages, 1781 KiB  
Article
Fluoroquinolones as Tyrosinase Inhibitors; Enzyme Kinetics and Molecular Docking Studies to Explore Their Mechanism of Action
by Bandar A. Alyami, Ali O. Alqarni, Yahya S. Alqahtani, Mater H. Mahnashi, Qamar Javed, Mubashir Hassan, Tehreem Tahir, Anser Ali, Katarzyna Kotwica-Mojzych and Mariusz Mojzych
Appl. Sci. 2022, 12(10), 4849; https://doi.org/10.3390/app12104849 - 11 May 2022
Cited by 3 | Viewed by 1797
Abstract
The binding of fluoroquinolones, the most commonly prescribed antibiotics, with melanin is well explored. However, their binding patterns and exact mechanism of interaction with tyrosinase, a key enzyme in melanogenesis, are not explored yet. Thus, in the present study, seven fluoroquinolone drugs were [...] Read more.
The binding of fluoroquinolones, the most commonly prescribed antibiotics, with melanin is well explored. However, their binding patterns and exact mechanism of interaction with tyrosinase, a key enzyme in melanogenesis, are not explored yet. Thus, in the present study, seven fluoroquinolone drugs were selected to characterize their interactions with the tyrosinase enzyme: ciprofloxacin, enoxacin sesquihydrate, ofloxacin, levofloxacin, sparfloxacin, moxifloxacin and gemifloxacin. The results confirmed that all the drugs execute excellent enzyme activity, with an inhibition range from IC50 = 28 ± 4 to 50 ± 1.9 μM, outperforming the standard hydroquinone (IC50 = 170 μM). Later, kinetic studies revealed that all the drugs showed irreversible, but mixed-type, tyrosinase inhibition, with a preferentially competitive mode of action. Further, 2D and 3D docked complexes and binding analyses confirmed their significant interactions in the active region of the target enzyme, sufficient for the downstream signaling responsible for the observed tyrosinase inhibition. Thus, this is the first report demonstrating their mechanism of tyrosinase inhibition, critical for melanin-dependent responses, including toxicity. Full article
(This article belongs to the Special Issue Heterocyclic Compounds with Potential Biological Activity - Volume II)
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16 pages, 4479 KiB  
Article
Promising Photocytotoxicity of Water-Soluble Phtalocyanine against Planktonic and Biofilm Pseudomonas aeruginosa Isolates from Lower Respiratory Tract and Chronic Wounds
by Wojciech Szczolko, Magdalena Ratajczak, Tomasz Koczorowski, Dorota Kaminska, Tomasz Goslinski and Jolanta Dlugaszewska
Appl. Sci. 2022, 12(8), 3707; https://doi.org/10.3390/app12083707 - 07 Apr 2022
Viewed by 1577
Abstract
Alternative methods of killing microbes have been extensively researched in connection with the widespread appearance of antibiotic resistance among pathogenic bacteria. In this study, we report on in vitro antimicrobial phototoxicity research of cationic phthalocyanine with 2-(4-N-methylmorpholin-4-ium-4-yl)ethoxy substituents against selected clinical strains of [...] Read more.
Alternative methods of killing microbes have been extensively researched in connection with the widespread appearance of antibiotic resistance among pathogenic bacteria. In this study, we report on in vitro antimicrobial phototoxicity research of cationic phthalocyanine with 2-(4-N-methylmorpholin-4-ium-4-yl)ethoxy substituents against selected clinical strains of Pseudomonas aeruginosa isolated from the lower respiratory tract and chronic wounds. The microorganisms tested in the research were analyzed in terms of drug resistance and biofilm formation. The photocytotoxic effect of phthalocyanine was determined by the reduction factor of bacteria. The studied cationic phthalocyanine at a concentration of 1.0 × 10−4 M, when activated by light, revealed a significant reduction factor, ranging from nearly 4 to 6 log, of P. aeruginosa cells when compared to the untreated control group. After single irradiation, a decrease in the number of bacteria in biofilm ranging from 1.3 to 4.2 log was observed, whereas the second treatment significantly improved the bacterial reduction factor from 3.4 to 5.5 log. It is worth mentioning that a boosted cell-death response was observed after the third irradiation, with a bacterial reduction factor ranging from 4.6 to 6.4 log. According to the obtained results, the tested photosensitizer can be considered as a potential antimicrobial photodynamic therapy against multidrug-resistant P. aeruginosa. Full article
(This article belongs to the Special Issue Heterocyclic Compounds with Potential Biological Activity - Volume II)
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6 pages, 521 KiB  
Communication
Synthesis and Structural Confirmation of the Thiazole Alkaloids Derived from Peganum harmala L.
by Myeonghyeon Sim, Sujin Lee and Youngtaek Han
Appl. Sci. 2022, 12(1), 78; https://doi.org/10.3390/app12010078 - 22 Dec 2021
Cited by 1 | Viewed by 2063
Abstract
Peganumal A and B are thiazole alkaloids isolated from the seeds of Peganum harmala L. Thiazole moieties are rarely found in natural products, but diverse compounds possessing thiazole moieties have attracted attention owing to their broad range of biological activities. Peganumals are the [...] Read more.
Peganumal A and B are thiazole alkaloids isolated from the seeds of Peganum harmala L. Thiazole moieties are rarely found in natural products, but diverse compounds possessing thiazole moieties have attracted attention owing to their broad range of biological activities. Peganumals are the first natural thiazole compounds isolated from the genus Peganum. It was difficult to define the exact structure of peganumal A via spectroscopic analysis. In this paper, we report the first total synthesis of peganumal A and B. The 5-benzylthiazole skeleton possessing methyl or hydrogen at the 2-position of the peganumals was efficiently constructed via the Hantzsch thiazole synthesis of the α-bromoaldehyde intermediate. Moreover, the spectral data of the synthetic 2H–thiazole compound were identical to those previously reported for peganumal A. The synthesis allowed the confirmation of the structure of peganumal A. Full article
(This article belongs to the Special Issue Heterocyclic Compounds with Potential Biological Activity - Volume II)
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Review

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31 pages, 5150 KiB  
Review
BODIPY-Based Nanomaterials—Sensing and Biomedical Applications
by Tomasz Koczorowski, Arleta Glowacka-Sobotta, Stepan Sysak, Dariusz T. Mlynarczyk, Roman Lesyk, Tomasz Goslinski and Lukasz Sobotta
Appl. Sci. 2022, 12(15), 7815; https://doi.org/10.3390/app12157815 - 03 Aug 2022
Cited by 7 | Viewed by 2568
Abstract
Cancerous diseases are rightfully considered among the most lethal, which have a consistently negative effect when considering official statistics in regular health reports around the globe. Nowadays, metallic nanoparticles can be potentially applied in medicine as active pharmaceuticals, adjustable carriers, or distinctive enhancers [...] Read more.
Cancerous diseases are rightfully considered among the most lethal, which have a consistently negative effect when considering official statistics in regular health reports around the globe. Nowadays, metallic nanoparticles can be potentially applied in medicine as active pharmaceuticals, adjustable carriers, or distinctive enhancers of physicochemical properties if combined with other drugs. Boron dipyrromethene (BODIPY) molecules have been considered for future applications in theranostics in the oncology field, thus expanding the potential of conceivable applicability. Hence, taking into account positive practical features of both metal-based nanostructures and BODIPY derivatives, the present study aims to gather recent results connected to BODIPY-conjugated metallic nanoparticles. This is with respect to their expediency in the diagnosis and treatment of tumor ailments as well as in sensing of heavy metals. To fulfill the designated objectives, multiple research documents were analyzed concerning the latest discoveries within the scope of BODIPY-based nanomaterials with particular emphasis on their utilization for diagnostical sensing as well as cancer diagnostics and therapy. In addition, collected examples of mentioned conjugates were presented in order to draw the attention of the scientific community to their practical applications, elucidate the topic in a consistent manner, and inspire fellow researchers for new findings. Full article
(This article belongs to the Special Issue Heterocyclic Compounds with Potential Biological Activity - Volume II)
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24 pages, 4260 KiB  
Review
Heterocyclic Crown Ethers with Potential Biological and Pharmacological Properties: From Synthesis to Applications
by Faiz Ullah, Taskin Aman Khan, Jawaria Iltaf, Saleha Anwar, Muhammad Farhan Ali Khan, Muhammad Rizwan Khan, Sami Ullah, Muhammad Fayyaz ur Rehman, Muhammad Mustaqeem, Katarzyna Kotwica-Mojzych and Mariusz Mojzych
Appl. Sci. 2022, 12(3), 1102; https://doi.org/10.3390/app12031102 - 21 Jan 2022
Cited by 19 | Viewed by 8596
Abstract
Cyclic organic compounds with several ether linkages in their structure are of much concern in our daily life applications. Crown ethers (CEs) are generally heterocyclic and extremely versatile compounds exhibiting higher binding affinity. In recent years, due to their unique structure, crown ethers [...] Read more.
Cyclic organic compounds with several ether linkages in their structure are of much concern in our daily life applications. Crown ethers (CEs) are generally heterocyclic and extremely versatile compounds exhibiting higher binding affinity. In recent years, due to their unique structure, crown ethers are widely used in drug delivery, solvent extraction, cosmetics manufacturing, material studies, catalysis, separation, and organic synthesis. Beyond their conventional place in chemistry, this review article summarizes the synthesis, biological, and potential pharmacological activities of CEs. We have emphasized the prospects of CEs as anticancer, anti-inflammatory, antibacterial, and antifungal agents and have explored their amyloid genesis inhibitory activity, electrochemical, and potential metric sensing properties. The central feature of these compounds is their ability to form selective and stable complexes with various organic and inorganic cations. Therefore, CEs can be used in gas chromatography as the stationary phase and are also valuable for cation chromatographic to determine and separate alkali and alkaline-earth cations. Full article
(This article belongs to the Special Issue Heterocyclic Compounds with Potential Biological Activity - Volume II)
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