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Advances in Medicinal Chemistry of Antibiotics
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Advances in Medicinal Chemistry of Antibiotics

A special issue of Molecules (ISSN 1420-3049).

Deadline for manuscript submissions: closed (31 August 2012) | Viewed by 57593

Special Issue Editor

Prof. Dr. Françoise Van Bambeke

E-Mail Website
Guest Editor
Pharmacologie Cellulaire et Moléculaire, Louvain Drug Research Institute, Université Catholique de Louvain, Avenue Mounier 73 B1.73.05, 1200 Brussels, Belgium
Interests: new antibiotics; pharmacokinetics and pharmacodynamics; intracellular infection; efflux transporters
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

In a world of increasing resistance, we have to urgently come with new, potent, weapons. Discovery of novel antibiotic classes acting on still unexploited targets remains a challenge. Another approach that has been followed quite intensively and successfully over the last years consists in refining our knowledge of structure-activity relationships to come with molecules showing an increased intrinsic activity, a reduced susceptibility to resistance mechanisms, an improved safety profile, or a better pharmacokinetic profile.
This special issue is aimed at presenting up-to-date reviews or promising experimental data on structure-activity relationships, either for existing classes of antibiotics or for new classes of antibiotics (meaning for which there is still no drug on the market).

Prof. Dr. Françoise Van Bambeke
Guest Editor

Keywords

  • structure-activity relationships
  • antibiotics
  • new antibacterial targets
  • activity towards multiresistant bacteria

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Published Papers (4 papers)

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Research

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28 pages, 456 KiB  
Article
Development of New Drugs for an Old Target — The Penicillin Binding Proteins
by Astrid Zervosen, Eric Sauvage, Jean-Marie Frère, Paulette Charlier and André Luxen
Molecules 2012, 17(11), 12478-12505; https://doi.org/10.3390/molecules171112478 - 24 Oct 2012
Cited by 89 | Viewed by 17590
Abstract
The widespread use of β-lactam antibiotics has led to the worldwide appearance of drug-resistant strains. Bacteria have developed resistance to β-lactams by two main mechanisms: the production of β-lactamases, sometimes accompanied by a decrease of outer membrane permeability, and the production of low-affinity, [...] Read more.
The widespread use of β-lactam antibiotics has led to the worldwide appearance of drug-resistant strains. Bacteria have developed resistance to β-lactams by two main mechanisms: the production of β-lactamases, sometimes accompanied by a decrease of outer membrane permeability, and the production of low-affinity, drug resistant Penicillin Binding Proteins (PBPs). PBPs remain attractive targets for developing new antibiotic agents because they catalyse the last steps of the biosynthesis of peptidoglycan, which is unique to bacteria, and lies outside the cytoplasmic membrane. Here we summarize the “current state of the art” of non-β-lactam inhibitors of PBPs, which have being developed in an attempt to counter the emergence of β-lactam resistance. These molecules are not susceptible to hydrolysis by β-lactamases and thus present a real alternative to β-lactams. We present transition state analogs such as boronic acids, which can covalently bind to the active serine residue in the catalytic site. Molecules containing ring structures different from the β-lactam-ring like lactivicin are able to acylate the active serine residue. High throughput screening methods, in combination with virtual screening methods and structure based design, have allowed the development of new molecules. Some of these novel inhibitors are active against major pathogens, including methicillin-resistant Staphylococcus aureus (MRSA) and thus open avenues new for the discovery of novel antibiotics. Full article
(This article belongs to the Special Issue Advances in Medicinal Chemistry of Antibiotics)
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9 pages, 192 KiB  
Article
Identification of Fungicidal 2,6-Disubstituted Quinolines with Activity against Candida Biofilms
by Nicolas Delattin, Dorothée Bardiot, Arnaud Marchand, Patrick Chaltin, Katrijn De Brucker, Bruno P. A. Cammue and Karin Thevissen
Molecules 2012, 17(10), 12243-12251; https://doi.org/10.3390/molecules171012243 - 18 Oct 2012
Cited by 10 | Viewed by 6971
Abstract
We have identified two subseries of 2,6-disubstituted quinolines, consisting of 6-amide and 6-urea derivatives, which are characterized by fungicidal activity against Candida albicans with minimal fungicidal concentration (MFC) values C. albicans, in particular compounds 1, 5 and 6 characterized by MFC values [...] Read more.
We have identified two subseries of 2,6-disubstituted quinolines, consisting of 6-amide and 6-urea derivatives, which are characterized by fungicidal activity against Candida albicans with minimal fungicidal concentration (MFC) values < 15 µM. The 6-amide derivatives displayed the highest fungicidal activity against C. albicans, in particular compounds 1, 5 and 6 characterized by MFC values of 6.25–12.5 µM. Compounds 1 and 5 of this series displayed fungicidal activity against the emerging pathogen Candida glabrata (MFC < 50 µM). The 6-amide derivatives 1, 2, 5, and 6 and the 6-urea derivatives 10, 12, 13 and 15 could also eradicate C. albicans biofilms. We found that the 6-urea derivatives 10, 13, and 15 induced accumulation of endogenous reactive oxygen species in Candida albicans biofilms. Full article
(This article belongs to the Special Issue Advances in Medicinal Chemistry of Antibiotics)
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13 pages, 273 KiB  
Article
Synthesis and Antibacterial Activities of Amphiphilic Neomycin B-based Bilipid Conjugates and Fluorinated Neomycin B-based Lipids
by Smritilekha Bera, Ramesh Dhondikubeer, Brandon Findlay, George G. Zhanel and Frank Schweizer
Molecules 2012, 17(8), 9129-9141; https://doi.org/10.3390/molecules17089129 - 2 Aug 2012
Cited by 27 | Viewed by 8017
Abstract
Investigating the effect of lipid hydrophobicity on the activity of amphiphilic neomycin B conjugates, six polycationic amphiphiles (PAs) were created. Four of the new compounds incorporated either palmitic or arachidic di-lipid lysine tails, while two had single fluorinated undecanoic acid tails. The basicity [...] Read more.
Investigating the effect of lipid hydrophobicity on the activity of amphiphilic neomycin B conjugates, six polycationic amphiphiles (PAs) were created. Four of the new compounds incorporated either palmitic or arachidic di-lipid lysine tails, while two had single fluorinated undecanoic acid tails. The basicity of half of the compounds was increased through the incorporation of six guanidine moieties, in order to assess the effect of base strength on antimicrobial activity. A panel of ten bacteria was used for the testing, with seven strains obtained from the American Type Culture Collection series and three clinical isolates from Canadian Intensive Care Units. When compared to previous results with hydrocarbon monolipids the PAs all compounds were found to have reduced activity, though the hemolytic activity of the compounds with fluorinated tails was sharply reduced, with only a moderate reduction in antimicrobial activity. Full article
(This article belongs to the Special Issue Advances in Medicinal Chemistry of Antibiotics)
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Review

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11 pages, 179 KiB  
Review
Antimicrobial Peptides for Therapeutic Applications: A Review
by Min-Duk Seo, Hyung-Sik Won, Ji-Hun Kim, Tsogbadrakh Mishig-Ochir and Bong-Jin Lee
Molecules 2012, 17(10), 12276-12286; https://doi.org/10.3390/molecules171012276 - 18 Oct 2012
Cited by 427 | Viewed by 23894
Abstract
Antimicrobial peptides (AMPs) have been considered as potential therapeutic sources of future antibiotics because of their broad-spectrum activities and different mechanisms of action compared to conventional antibiotics. Although AMPs possess considerable benefits as new generation antibiotics, their clinical and commercial development still have [...] Read more.
Antimicrobial peptides (AMPs) have been considered as potential therapeutic sources of future antibiotics because of their broad-spectrum activities and different mechanisms of action compared to conventional antibiotics. Although AMPs possess considerable benefits as new generation antibiotics, their clinical and commercial development still have some limitations, such as potential toxicity, susceptibility to proteases, and high cost of peptide production. In order to overcome those obstacles, extensive efforts have been carried out. For instance, unusual amino acids or peptido-mimetics are introduced to avoid the proteolytic degradation and the design of short peptides retaining antimicrobial activities is proposed as a solution for the cost issue. In this review, we focus on small peptides, especially those with less than twelve amino acids, and provide an overview of the relationships between their three-dimensional structures and antimicrobial activities. The efforts to develop highly active AMPs with shorter sequences are also described. Full article
(This article belongs to the Special Issue Advances in Medicinal Chemistry of Antibiotics)
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