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Antibiotics
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Searching for Small Molecules as Antimicrobials
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Searching for Small Molecules as Antimicrobials

A special issue of Antibiotics (ISSN 2079-6382). This special issue belongs to the section "Novel Antimicrobial Agents".

Deadline for manuscript submissions: closed (31 March 2023) | Viewed by 21132

Special Issue Editor

Prof. Dr. Alessia Catalano

E-Mail Website
Guest Editor
Dipartimento di Farmacia, Scienze del Farmaco, Università di Bari, Bari, Italy
Interests: antibacterials; antifungals; antitumor agents; medicinal chemistry; toxicology; small molecules; antimyotonic agents
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Antimicrobial resistance is a growing problem in the treatment of infectious diseases, as it restricts antimicrobials’ efficacy in nearly every infection. However, the population-level consumption of these drugs has not decreased, due to their undisputed usefulness. Currently, the treatment and prevention of COVID-19, caused by novel coronavirus SARS-CoV-2, involves the use of antimicrobials. Therefore, there is an urgent need for the development of new, effective, broad-spectrum antimicrobial agents. Small molecules have gained great attention in the past two decades because of their remarkable advantages, such as low weight, ease of synthesis, low cost, and flexibility. They are widely used as tools for novel drugs; therefore, small molecules and small-molecule-containing drugs are certain to play an increasingly important role in medicinal chemistry. This Special Issue seeks manuscript submissions that can improve the existing knowledge about small molecules as antimicrobial agents.

Prof. Dr. Alessia Catalano
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. Antibiotics 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 2900 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

  • Small molecules
  • antimicrobials
  • COVID-19
  • antimicrobial resistance
  • antibacterials
  • antifungal
  • antiviral
  • antiprasitic
  • drug discovery
  • bioactive molecules
  • biofilms
  • Plant antimicrobial peptides

Published Papers (7 papers)

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Research

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10 pages, 417 KiB  
Article
Virucidal Activity of Lemon Essential Oil against Feline Calicivirus Used as Surrogate for Norovirus
by Francesco Pellegrini, Michele Camero, Cristiana Catella, Giuseppe Fracchiolla, Sabina Sblano, Giovanni Patruno, Claudia Maria Trombetta, Michela Galgano, Annamaria Pratelli, Maria Tempesta, Vito Martella and Gianvito Lanave
Antibiotics 2023, 12(2), 322; https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics12020322 - 03 Feb 2023
Cited by 3 | Viewed by 1729
Abstract
Norovirus (NoV) is regarded as a common cause of acute gastrointestinal illness worldwide in all age groups, with substantial morbidity across health care and community settings. The lack of in vitro cell culture systems for human NoV has prompted the use of cultivatable [...] Read more.
Norovirus (NoV) is regarded as a common cause of acute gastrointestinal illness worldwide in all age groups, with substantial morbidity across health care and community settings. The lack of in vitro cell culture systems for human NoV has prompted the use of cultivatable caliciviruses (such as feline calicivirus, FCV, or murine NoV) as surrogates for in vitro evaluation of antivirals. Essential oils (EOs) may represent a valid tool to counteract viral infections, particularly as food preservatives. In the present study, the virucidal efficacy of lemon EO (LEO) against FCV was assessed in vitro. The gas chromatography hyphenated with mass spectrometry (GC/MS) technique was used to reveal the chemical composition of LEO. The following small molecules were detected as major components of LEO: limonene (53%), β-pinene (14.5%), γ-terpinene (5.9%), citral (3.8%), α-pinene (2.4%), and β-thujene (1.94%). LEO at 302.0 μg/mL, exceeding the maximum non cytotoxic limit, significantly decreased viral titre of 0.75 log10 TCID50/50 μL after 8 h. Moreover, virucidal activity was tested using LEO at 3020.00 μg/mL, determining a reduction of viral titre as high as 1.25 log10 TCID50/50 μL after 8 h of time contact. These results open up perspectives for the development of alternative prophylaxis approaches for the control of NoV infection. Full article
(This article belongs to the Special Issue Searching for Small Molecules as Antimicrobials)
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11 pages, 829 KiB  
Article
Antibacterial, Antibiofilm and Anti-Virulence Activity of Biactive Fractions from Mucus Secretion of Giant African Snail Achatina fulica against Staphylococcus aureus Strains
by Libardo Suárez, Andrés Pereira, William Hidalgo and Nelson Uribe
Antibiotics 2021, 10(12), 1548; https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics10121548 - 17 Dec 2021
Cited by 9 | Viewed by 3188
Abstract
Staphylococcus aureus is an important etiological agent that causes skin infections, and has the propensity to form biofilms, leading to significant mortality and morbidity in patients with wounds. Mucus secretion from the Giant African snail Achatina fulica is a potential source of biologically [...] Read more.
Staphylococcus aureus is an important etiological agent that causes skin infections, and has the propensity to form biofilms, leading to significant mortality and morbidity in patients with wounds. Mucus secretion from the Giant African snail Achatina fulica is a potential source of biologically active substances that might be an important source for new drugs to treat resistant and biofilm-forming bacteria such as S. aureus. This study evaluated the effect of semi-purified fractions from the mucus secretion of A. fulica on the growth, biofilm formation and virulence factors of S. aureus. Two fractions: FMA30 (Mw >30 kDa) and FME30 (Mw 30−10 kDa) exhibited antimicrobial activity against S. aureus with a MIC50 of 25 and 125 µg/mL, respectively. An inhibition of biofilm formation higher than 80% was observed at 9 µg/mL with FMA30 and 120 µg/mL with FME30. Furthermore, inhibition of hemolytic and protease activity was determined using a concentration of MIC20, and FME30 showed a strong inhibitory effect in the formation of clots. We report for the first time the effect of semi-purified fractions of mucus secretion of A. fulica on biofilm formation and activity of virulence factors such as α-hemolysin, coagulase and proteases produced by S. aureus strains. Full article
(This article belongs to the Special Issue Searching for Small Molecules as Antimicrobials)
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12 pages, 2451 KiB  
Article
Benzothiazole-Containing Analogues of Triclocarban with Potent Antibacterial Activity
by Alessia Catalano, Antonio Rosato, Lara Salvagno, Domenico Iacopetta, Jessica Ceramella, Giuseppe Fracchiolla, Maria Stefania Sinicropi and Carlo Franchini
Antibiotics 2021, 10(7), 803; https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics10070803 - 01 Jul 2021
Cited by 14 | Viewed by 2268
Abstract
Triclocarban (TCC) is a polychlorinated, aromatic, antimicrobial agent commercially used since the 1950s in personal care products for the prevention of spoilage and infections. Humans are frequently exposed to TCC due to its widespread use, leading to its substantial release into the aquatic [...] Read more.
Triclocarban (TCC) is a polychlorinated, aromatic, antimicrobial agent commercially used since the 1950s in personal care products for the prevention of spoilage and infections. Humans are frequently exposed to TCC due to its widespread use, leading to its substantial release into the aquatic environment. With the recent ban of TCC from some personal care products, implemented in 2016, many replacement antimicrobial compounds have been studied by researchers. Herein, we report the synthesis and biological activity of a series of diarylureas, analogues of TCC that bear the benzothiazole nucleus as one of the two aryl moieties. Among the studied compounds, 2bF and 2eC showed the highest antimicrobial activity against Staphylococcus aureus, being also more active than TCC, with MIC values of 8 µg/mL versus 16 µg/mL of TCC. Moreover, compound 2bB was much more active than TCC against Enterococcus faecalis, a Gram-positive bacterium that is, unfortunately, strongly responsible for nosocomial infections. Finally, interesting results were found for compound 2bG that, even though less active than the others, exerts an interesting bactericidal action. Full article
(This article belongs to the Special Issue Searching for Small Molecules as Antimicrobials)
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Review

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18 pages, 1344 KiB  
Review
Sugar-Based Monoester Surfactants: Synthetic Methodologies, Properties, and Biological Activities
by Michele Verboni, Diego Romano Perinelli, Alessandro Buono, Raffaella Campana, Maurizio Sisti, Andrea Duranti and Simone Lucarini
Antibiotics 2023, 12(10), 1500; https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics12101500 - 30 Sep 2023
Cited by 1 | Viewed by 1107
Abstract
Glycolipids are biocompatible and biodegradable amphiphilic compounds characterized by a great scientific interest for their potential applications in various technological areas, including pharmaceuticals, cosmetics, agriculture, and food production. This report summarizes the available synthetic methodologies, physicochemical properties, and biological activity of sugar fatty [...] Read more.
Glycolipids are biocompatible and biodegradable amphiphilic compounds characterized by a great scientific interest for their potential applications in various technological areas, including pharmaceuticals, cosmetics, agriculture, and food production. This report summarizes the available synthetic methodologies, physicochemical properties, and biological activity of sugar fatty acid ester surfactants, with a particular focus on 6-O-glucose, 6-O-mannose, 6-O-sucrose, and 6′-O-lactose ones. In detail, the synthetic approaches to this class of compounds, such as enzymatic lipase-catalyzed and traditional chemical (e.g., acyl chloride, Steglich, Mitsunobu) esterifications, are reported. Moreover, aspects related to the surface activity of these amphiphiles, such as their ability to decrease surface tension, critical micelle concentration, and emulsifying and foaming ability, are described. Biological applications with a focus on the permeability-enhancing effect across the skin or mucosa, antimicrobial and antifungal activities, as well as antibiofilm properties, are also presented. The information reported here on sugar-based ester surfactants is helpful to broaden the interest and the possible innovative applications of this class of amphiphiles in different technological fields in the future. Full article
(This article belongs to the Special Issue Searching for Small Molecules as Antimicrobials)
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13 pages, 3546 KiB  
Review
Diarylureas: New Promising Small Molecules against Streptococcus mutans for the Treatment of Dental Caries
by Domenico Iacopetta, Jessica Ceramella, Alessia Catalano, Assunta D’Amato, Graziantonio Lauria, Carmela Saturnino, Inmaculada Andreu, Pasquale Longo and Maria Stefania Sinicropi
Antibiotics 2023, 12(1), 112; https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics12010112 - 07 Jan 2023
Cited by 4 | Viewed by 3309
Abstract
Dental caries is a biofilm-mediated disease that represents a worldwide oral health issue. Streptococcus mutans has been ascertained as the main cariogenic pathogen responsible for human dental caries, with a high ability to form biofilms, regulated by the quorum sensing. Diarylureas represent a [...] Read more.
Dental caries is a biofilm-mediated disease that represents a worldwide oral health issue. Streptococcus mutans has been ascertained as the main cariogenic pathogen responsible for human dental caries, with a high ability to form biofilms, regulated by the quorum sensing. Diarylureas represent a class of organic compounds that show numerous biological activities, including the antimicrobial one. Two small molecules belonging to this class, specifically to diphenylureas, BPU (1,3-bis[3,5-bis(trifluoromethyl)phenyl]urea) and DMTU (1,3-di-m-tolyl-urea), showed interesting results in studies regarding the antimicrobial activity against the cariogenic bacterium S. mutans. Since there are not many antimicrobials used for the prevention and treatment of caries, further studies on these two interesting compounds and other diarylureas against S. mutans may be useful to design new effective agents for the treatment of caries with generally low cytotoxicity. Full article
(This article belongs to the Special Issue Searching for Small Molecules as Antimicrobials)
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14 pages, 2381 KiB  
Review
Thidiazuron: New Trends and Future Perspectives to Fight Xylella fastidiosa in Olive Trees
by Alessia Catalano, Jessica Ceramella, Domenico Iacopetta, Annaluisa Mariconda, Elisabetta Scali, Maria Grazia Bonomo, Carmela Saturnino, Pasquale Longo, Stefano Aquaro and Maria Stefania Sinicropi
Antibiotics 2022, 11(7), 947; https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics11070947 - 14 Jul 2022
Cited by 6 | Viewed by 2497
Abstract
These days, most of our attention has been focused on the COVID-19 pandemic, and we have often neglected what is happening in the environment. For instance, the bacterium Xylella fastidiosa re-emerged as a plant pathogen of global importance in 2013 when it was [...] Read more.
These days, most of our attention has been focused on the COVID-19 pandemic, and we have often neglected what is happening in the environment. For instance, the bacterium Xylella fastidiosa re-emerged as a plant pathogen of global importance in 2013 when it was first associated with an olive tree disease epidemic in Italy, called Olive Quick Decline Syndrome (OQDS), specifically caused by X. fastidiosa subspecies pauca ST53, which affects the Salento olive trees (Apulia, South-East Italy). This bacterium, transmitted by the insect Philaenus spumarius, is negatively reshaping the Salento landscape and has had a very high impact in the production of olives, leading to an increase of olive oil prices, thus new studies to curb this bacterium are urgently needed. Thidiazuron (TDZ), a diphenylurea (N-phenyl-1,2,3-thiadiazol-5-yl urea), has gained considerable attention in recent decades due to its efficient role in plant cell and tissue culture, being the most suitable growth regulator for rapid and effective plant production in vitro. Its biological activity against bacteria, fungi and biofilms has also been described, and the use of this low-cost compound to fight OQDS may be an intriguing idea. Full article
(This article belongs to the Special Issue Searching for Small Molecules as Antimicrobials)
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28 pages, 1941 KiB  
Review
Triclosan: A Small Molecule with Controversial Roles
by Maria Stefania Sinicropi, Domenico Iacopetta, Jessica Ceramella, Alessia Catalano, Annaluisa Mariconda, Michele Pellegrino, Carmela Saturnino, Pasquale Longo and Stefano Aquaro
Antibiotics 2022, 11(6), 735; https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics11060735 - 30 May 2022
Cited by 21 | Viewed by 5804
Abstract
Triclosan (TCS), a broad-spectrum antimicrobial agent, has been widely used in personal care products, medical products, plastic cutting boards, and food storage containers. Colgate Total® toothpaste, containing 10 mM TCS, is effective in controlling biofilm formation and maintaining gingival health. Given its [...] Read more.
Triclosan (TCS), a broad-spectrum antimicrobial agent, has been widely used in personal care products, medical products, plastic cutting boards, and food storage containers. Colgate Total® toothpaste, containing 10 mM TCS, is effective in controlling biofilm formation and maintaining gingival health. Given its broad usage, TCS is present ubiquitously in the environment. Given its strong lipophilicity and accumulation ability in organisms, it is potentially harmful to biohealth. Several reports suggest the toxicity of this compound, which is inserted in the class of endocrine disrupting chemicals (EDCs). In September 2016, TCS was banned by the U.S. Food and Drug Administration (FDA) and the European Union in soap products. Despite these problems, its application in personal care products within certain limits is still allowed. Today, it is still unclear whether TCS is truly toxic to mammals and the adverse effects of continuous, long-term, and low concentration exposure remain unknown. Indeed, some recent reports suggest the use of TCS as a repositioned drug for cancer treatment and cutaneous leishmaniasis. In this scenario it is necessary to investigate the advantages and disadvantages of TCS, to understand whether its use is advisable or not. This review intends to highlight the pros and cons that are associated with the use of TCS in humans. Full article
(This article belongs to the Special Issue Searching for Small Molecules as Antimicrobials)
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