{"title":"1,2,3-Triazole‑gold(I)-triethylphosphine derivatives of nutrients as new antimicrobials against antibiotic resistant Gram-positive pathogens","authors":"Mathieu Michaut , Françoise Hoegy , Alexandre Steffen , Jean-Marie Contreras , Christophe Morice , Patrick Plésiat , Gaëtan L.A. Mislin","doi":"10.1016/j.bmcl.2025.130276","DOIUrl":null,"url":null,"abstract":"<div><div>The ongoing rise of bacterial resistance against antibiotics is an incentive to develop radically new antibacterial molecules. Innovative organo-gold(I) antibacterial compounds were synthesized by click chemistry with triethylphosphine‑gold(I) azides and alkyne-functionalized metabolites like amino acids, nicotinic acid and biotin. The resulting organo‑gold(I) compounds exhibited remarkable activities against a panel of Gram-positive pathogens (<em>Staphyloccocus sp</em>., <em>Enterococcus sp</em>. and <em>Clostridium difficile</em>) but failed to inhibit the growth of Gram-negative bacilli (e.g., <em>Escherichia coli</em>) under the conditions used (8 μg. mL<sup>−1</sup> maximum).</div></div>","PeriodicalId":256,"journal":{"name":"Bioorganic & Medicinal Chemistry Letters","volume":"125 ","pages":"Article 130276"},"PeriodicalIF":2.5000,"publicationDate":"2025-05-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Bioorganic & Medicinal Chemistry Letters","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0960894X25001854","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0
Abstract
The ongoing rise of bacterial resistance against antibiotics is an incentive to develop radically new antibacterial molecules. Innovative organo-gold(I) antibacterial compounds were synthesized by click chemistry with triethylphosphine‑gold(I) azides and alkyne-functionalized metabolites like amino acids, nicotinic acid and biotin. The resulting organo‑gold(I) compounds exhibited remarkable activities against a panel of Gram-positive pathogens (Staphyloccocus sp., Enterococcus sp. and Clostridium difficile) but failed to inhibit the growth of Gram-negative bacilli (e.g., Escherichia coli) under the conditions used (8 μg. mL−1 maximum).
期刊介绍:
Bioorganic & Medicinal Chemistry Letters presents preliminary experimental or theoretical research results of outstanding significance and timeliness on all aspects of science at the interface of chemistry and biology and on major advances in drug design and development. The journal publishes articles in the form of communications reporting experimental or theoretical results of special interest, and strives to provide maximum dissemination to a large, international audience.