Antimycobacterial Agents: Combating Drug-Resistant Tuberculosis

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (30 April 2023) | Viewed by 2982

Special Issue Editor


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Guest Editor
Faculty of Health Sciences, Curtin Medical School, Curtin University, Perth, Australia
Interests: medicinal chemistry; structure–activity relationship; privileged scaffold; novel synthetic methodology; mycobacteria; cannabinoids; brain cancer; neurodegeneration; neuroinflammation

Special Issue Information

Dear Colleagues,

Tuberculosis (TB) remained the leading cause of death caused by infection until it was overtaken by SARS-CoV-2. The causative agent, Mycobacterium tuberculosis, is known to be highly effective in staying dormant within the human host, and when the time is right—often coinciding with the host’s immune system being compromised—it will cause the development of the disease phenotype. Similarly to what we have witnessed with the resistance observed for COVID-19 variants, multi-drug- and extensively drug-resistant forms of TB necessitate novel treatment and preventative options. A lot still needs to be uncovered regarding aspects of TB host–bacteria interplay and combating the resistant forms. The vaccine has played a key role in providing immunity worldwide since its discovery around a century ago. However, much like what we have seen with COVID-19 vaccines, both preventative and treatment options are crucial for healthcare. This is when medicinal chemists and pharmacologists from academic, open-source and pharma settings have a role to play: small-molecule drugs will continue to provide essential ammunition for human medicine.     With this background in mind, I would like to invite you to contribute towards our Special Issue entitled “Antimycobacterial Agents: Combating Drug-Resistant Tuberculosis” with Pharmaceutics (IF = 5.215). The following points represent broad areas of interest that papers submitted to this Special Issue may cover: 

  • All aspects within the definition of medicinal chemistry related to the invention, discovery, design, identification and preparation of antimycobacterial compounds, the study of their binding and/or functional activities, metabolism/ADMET, the interpretation of their mode of action at the molecular level and the construction of structure–activity relationships;
  • Novel strategies and synthetic methodologies with relevant application to mycobacterial chemical biology and medicinal chemistry;
  • We aim to publish updated reviews as well as research articles with comprehensive theoretical and experimental details covering all aspects of small molecules as drug candidates, e.g., drug discovery and design, combinatorial chemistry, structure-property correlations, molecular modelling and bioinformatics. Short communications are also accepted; therefore, there is no restriction on the length of a paper.

 I look forward to receiving your exciting scientific findings.

Dr. Hendra Gunosewoyo
Guest Editor

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Keywords

  • medicinal chemistry
  • structure–activity relationship
  • genomics
  • transcriptomics
  • proteomics
  • mycobacteria
  • tuberculosis
  • drug resistance
  • latent tuberculosis
  • Mycobacterium abscessus
  • drug repurposing

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Published Papers (1 paper)

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Research

27 pages, 9236 KiB  
Article
Exploring the Antitubercular Activity of Anthranilic Acid Derivatives: From MabA (FabG1) Inhibition to Intrabacterial Acidification
by Léo Faïon, Kamel Djaout, Catalin Pintiala, Catherine Piveteau, Florence Leroux, Alexandre Biela, Stéphanie Slupek, Rudy Antoine, Monika Záhorszká, Francois-Xavier Cantrelle, Xavier Hanoulle, Jana Korduláková, Benoit Deprez, Nicolas Willand, Alain R. Baulard and Marion Flipo
Pharmaceuticals 2023, 16(3), 335; https://doi.org/10.3390/ph16030335 - 22 Feb 2023
Cited by 3 | Viewed by 2552
Abstract
Mycobacterium tuberculosis, the pathogen that causes tuberculosis, is responsible for the death of 1.5 million people each year and the number of bacteria resistant to the standard regimen is constantly increasing. This highlights the need to discover molecules that act on new [...] Read more.
Mycobacterium tuberculosis, the pathogen that causes tuberculosis, is responsible for the death of 1.5 million people each year and the number of bacteria resistant to the standard regimen is constantly increasing. This highlights the need to discover molecules that act on new M. tuberculosis targets. Mycolic acids, which are very long-chain fatty acids essential for M. tuberculosis viability, are synthesized by two types of fatty acid synthase (FAS) systems. MabA (FabG1) is an essential enzyme belonging to the FAS-II cycle. We have recently reported the discovery of anthranilic acids as MabA inhibitors. Here, the structure–activity relationships around the anthranilic acid core, the binding of a fluorinated analog to MabA by NMR experiments, the physico-chemical properties and the antimycobacterial activity of these inhibitors were explored. Further investigation of the mechanism of action in bacterio showed that these compounds affect other targets than MabA in mycobacterial cells and that their antituberculous activity is due to the carboxylic acid moiety which induces intrabacterial acidification. Full article
(This article belongs to the Special Issue Antimycobacterial Agents: Combating Drug-Resistant Tuberculosis)
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