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Discovery of Antibacterial Drugs
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Discovery of Antibacterial Drugs

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

Deadline for manuscript submissions: 30 April 2025 | Viewed by 2341

Special Issue Editor

Prof. Dr. Pavlina Dolashka

E-Mail Website
Guest Editor
Institute of Organic Chemistry with Centre of Phytochemistry, Bulgarian Academy of Sciences, Str. G. Bonchev 9, 1113 Sofia, Bulgaria
Interests: biochemistry; polysaccharide; glycoproteins; nanoparticle; biomedicine; structural and functional investigations on proteins with biomedical and industrial importance; isolation and purification of proteins, antibiotics, proteinases, inhibitors and hemocyanins; investigations on the reactivity of functional groups in proteinases, hemocyanins and their role in catalysis; stability of proteinases in the presence of denaturing agents; spectroscopic studies on the structure in solution of proteins: absorption, emission spectroscopy and circular dichroism; kinetic investigations on the mechanism of enzymes; structure and function of oxygen-transporting proteins in invertebrates (hemocyanins and superoxide dismutases)
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

We invite the submissions of reviews and original scientific articles related to the field of antibacterial drug discovery. Eligible studies should represent innovative discoveries for the design and development of new antibacterial drugs with regard to the treatment of various bacterial infections. Moreover, studies on the increasing antimicrobial resistance that is causing the deaths of many people, caused by drug-susceptible bacterial infections, are also of interest.

Furthermore, research on molecular modeling, molecular dynamics, etc., which contribute to the design and elucidation of drug action, is encouraged. Studies on natural compounds, the chemical structure of drugs, and the influence on their pharmacodynamic and pharmacokinetic characteristics are also welcome.

We invite eminent and young academics from around the world to submit papers to this Special Issue.

Prof. Dr. Pavlina Dolashka
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

  • antibacterial effect
  • antibiotics
  • drug discovery
  • natural compounds
  • pharmacodynamic and pharmacokinetic characteristics

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Published Papers (3 papers)

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Research

28 pages, 11822 KiB  
Article
Synthesis and Characterization of Magnesium Oxide-Enhanced Chitosan-Based Hemostatic Gels with Antibacterial Properties: Role of Amino Acids and Crosslinking
by Julia Radwan-Pragłowska, Paulina Bąk, Łukasz Janus, Aleksandra Sierakowska-Byczek, Piotr Radomski, Agnieszka Kramek, Justyna Gumieniak and Dariusz Bogdał
Molecules 2025, 30(7), 1496; https://doi.org/10.3390/molecules30071496 - 27 Mar 2025
Viewed by 224
Abstract
Excessive blood loss is a leading cause of mortality among soldiers and accident victims. The wound healing process typically ranges from three weeks to several months, with disruptions in healing stages potentially prolonging recovery time. Chronic wounds may persist for years, creating a [...] Read more.
Excessive blood loss is a leading cause of mortality among soldiers and accident victims. The wound healing process typically ranges from three weeks to several months, with disruptions in healing stages potentially prolonging recovery time. Chronic wounds may persist for years, creating a favorable environment for microbial growth. Chitosan, a derivative of chitin—the second most abundant biopolymer in nature—is obtained through deacetylation and exhibits mucoadhesive, analgesic, antioxidant, biodegradable, non-toxic, and biocompatible properties. Due to its hemostatic and regenerative support capabilities, chitosan is widely applied in the food, cosmetic, and agricultural industries; environmental protection; and as a key component in dressings for chronic wound healing. Notably, its antibacterial properties make it a promising candidate for novel biomaterials to replace traditional antibiotics and prevent the emergence of drug-resistant strains. The primary aim of this study was the chemical cross-linking of chitosan with the amino acids L-aspartic and L-glutamic acid in the presence of periclase (magnesium oxide) under microwave radiation conditions. Subsequent research stages involved the analysis of the samples’ physicochemical properties using SEM, FT-IR, XPS, atomic absorption spectrometry, swelling behavior (in water, SBF, and blood), porosity, and density. Biological assessments included biodegradation, cytotoxicity, and antibacterial activity against Escherichia coli and Staphylococcus aureus. The obtained results confirmed the high potential of the newly developed hemostatic agents for effective hemorrhage management under non-sterile conditions. Full article
(This article belongs to the Special Issue Discovery of Antibacterial Drugs)
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25 pages, 7568 KiB  
Article
Green Synthesis of Antibacterial CuO Nanoparticles Based on the Synergy Between Cornu aspersum Snail Mucus and Ascorbic Acid
by Maria Todorova, Angelina Kosateva, Ventsislava Petrova, Bogdan Ranguelov, Stela Atanasova-Vladimirova, Georgi Avdeev, Ivanka Stoycheva, Emiliya Pisareva, Anna Tomova, Lyudmila Velkova, Aleksandar Dolashki and Pavlina Dolashka
Molecules 2025, 30(2), 291; https://doi.org/10.3390/molecules30020291 - 13 Jan 2025
Viewed by 782
Abstract
Many biologically active compounds have been identified in the mucus of the garden snail Cornu aspersum, which are effective in the treatment of several diseases such as cancer, ulcers, wounds, etc. The incorporation of these compounds into the green synthesis of copper [...] Read more.
Many biologically active compounds have been identified in the mucus of the garden snail Cornu aspersum, which are effective in the treatment of several diseases such as cancer, ulcers, wounds, etc. The incorporation of these compounds into the green synthesis of copper nanoparticles (CuONPs-Muc) was demonstrated in our previous study. Based on the synergistic effect of two reducing agents—C. aspersum snail mucus and ascorbic acid (AsA)—on CuSO4.5H2O, which also act as stabilizers of the resulting compound, a new method for the “green” synthesis of CuONPs-Muc is presented. Using two reducing agents has several advantages, such as forming spherical nanoparticles with a diameter of about 150 nm and reducing the formation time of CuONPs-Muc to 3 h. Analyses by ultraviolet–visible spectroscopy (UV-Vis) and Fourier transform infrared spectroscopy (FT-IR) show the formation of CuONPs-Muc, composed of a mixture of copper and copper oxide. This was confirmed by scanning electron microscopy combined with energy-dispersive spectroscopy (SEM/EDS) and X-ray diffraction (XRD). Another important advantage of CuONPs obtained by the new method with two reducing agents is the stronger inhibitory effect on the bacterial growth of some Gram-positive and Gram-negative bacterial strains, compared to CuONPs-Muc prepared with only one reducing agent, i.e., a fraction of mucus with an MW > 20 kDa. Full article
(This article belongs to the Special Issue Discovery of Antibacterial Drugs)
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17 pages, 3408 KiB  
Article
Thiosemicarbazone-Based Compounds: A Promising Scaffold for Developing Antibacterial, Antioxidant, and Anticancer Therapeutics
by Agnieszka Czylkowska, Monika Pitucha, Anita Raducka, Ewelina Fornal, Edyta Kordialik-Bogacka, Sylwia Ścieszka, Marek Smoluch, Franciszek Burdan, Mateusz Jędrzejec and Paweł Szymański
Molecules 2025, 30(1), 129; https://doi.org/10.3390/molecules30010129 - 31 Dec 2024
Viewed by 1199
Abstract
This paper presents the synthesis and characterization of new thiosemicarbazone derivatives with potential applications as antibacterial, antioxidant and anticancer agents. Six thiosemicarbazone derivatives (L–L5) were synthesized by reacting an appropriate thiosemicarbazide derivative with 2-pyridinecarboxaldehyde. The structures of the obtained compounds were confirmed using [...] Read more.
This paper presents the synthesis and characterization of new thiosemicarbazone derivatives with potential applications as antibacterial, antioxidant and anticancer agents. Six thiosemicarbazone derivatives (L–L5) were synthesized by reacting an appropriate thiosemicarbazide derivative with 2-pyridinecarboxaldehyde. The structures of the obtained compounds were confirmed using mass spectrometry, infrared spectroscopy, and NMR spectroscopy. Antibacterial activity was evaluated by using the microdilution method, determining the minimum inhibitory concentration (MIC) against a panel of Gram-positive and Gram-negative bacteria. Compound L1 showed the most potent antibacterial activity, especially against Bacillus cereus (MIC 10 mg/L). Molecular docking to topoisomerase II and transcriptional regulator PrfA suggests that the studied compounds can effectively bind to molecular targets recognized in anticancer and antibacterial therapies. An assessment of physicochemical properties (ADME) indicates favorable parameters of the compounds as potential drugs. Compounds L and L2 showed the highest antioxidant activity, surpassing the activity of the Trolox standard. Cytotoxicity against A549 lung cancer cells was evaluated by the MTT assay. Compound L4 exhibited the strongest inhibitory effect on cancer cell survival. The obtained results indicate that the synthesized thiosemicarbazide derivatives, especially L1, L2, and L4, are promising compounds with potential applications as antibacterial and anticancer drugs. Full article
(This article belongs to the Special Issue Discovery of Antibacterial Drugs)
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