{"title":"Systematic Review on 1,2,3-Oxadiazoles, 1,2,4-Oxadiazoles, and 1,2,5-Oxadiazoles in the Antimycobacterial Drug Discovery.","authors":"Marta Kučerová-Chlupáčová","doi":"10.1002/cmdc.202400971","DOIUrl":null,"url":null,"abstract":"<p><p>Tuberculosis remains a leading global health threat, exacerbated by the emergence of multi-drug-resistant strains. The search for novel therapeutic agents is critical in addressing this challenge. This review systematically summarizes the potential of oxadiazole derivatives as promising candidates in antimycobacterial drug discovery. We focus on various classes of oxadiazoles, especially 1,2,3-oxadiazoles, 1,2,4-oxadiazoles, and 1,2,5-oxadiazoles, highlighting their structural diversity and biological activities. Recent advancements in structure-activity relationship studies are discussed, emphasizing the mechanisms of antimycobacterial action. Additionally, the synergistic potential of 1,2,4-oxadiazoles in enhancing the efficacy of existing tuberculosis treatment with ethionamide is also discussed. By integrating insights from recent research, this review aims to provide a comprehensive overview of the role of oxadiazoles in the fight against tuberculosis, paving the way for future investigations and the development of effective therapeutic strategies.</p>","PeriodicalId":147,"journal":{"name":"ChemMedChem","volume":" ","pages":"e202400971"},"PeriodicalIF":3.6000,"publicationDate":"2025-01-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"ChemMedChem","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1002/cmdc.202400971","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
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Abstract
Tuberculosis remains a leading global health threat, exacerbated by the emergence of multi-drug-resistant strains. The search for novel therapeutic agents is critical in addressing this challenge. This review systematically summarizes the potential of oxadiazole derivatives as promising candidates in antimycobacterial drug discovery. We focus on various classes of oxadiazoles, especially 1,2,3-oxadiazoles, 1,2,4-oxadiazoles, and 1,2,5-oxadiazoles, highlighting their structural diversity and biological activities. Recent advancements in structure-activity relationship studies are discussed, emphasizing the mechanisms of antimycobacterial action. Additionally, the synergistic potential of 1,2,4-oxadiazoles in enhancing the efficacy of existing tuberculosis treatment with ethionamide is also discussed. By integrating insights from recent research, this review aims to provide a comprehensive overview of the role of oxadiazoles in the fight against tuberculosis, paving the way for future investigations and the development of effective therapeutic strategies.
期刊介绍：
Quality research. Outstanding publications. With an impact factor of 3.124 (2019), ChemMedChem is a top journal for research at the interface of chemistry, biology and medicine. It is published on behalf of Chemistry Europe, an association of 16 European chemical societies.
ChemMedChem publishes primary as well as critical secondary and tertiary information from authors across and for the world. Its mission is to integrate the wide and flourishing field of medicinal and pharmaceutical sciences, ranging from drug design and discovery to drug development and delivery, from molecular modeling to combinatorial chemistry, from target validation to lead generation and ADMET studies. ChemMedChem typically covers topics on small molecules, therapeutic macromolecules, peptides, peptidomimetics, and aptamers, protein-drug conjugates, nucleic acid therapies, and beginning 2017, nanomedicine, particularly 1) targeted nanodelivery, 2) theranostic nanoparticles, and 3) nanodrugs.
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ChemMedChem publishes an attractive mixture of:
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