{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Sorokin B"],"funding":["Ministry of Science and Higher Education of the Russian Federation"],"pagination":["1870"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC11899342"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["26(5)"],"pubmed_abstract":["Bacterial antibiotic resistance represents a major healthcare problem. In 2019, 4.95 million deaths were associated with antibiotic resistance, and it is estimated that, by 2050, up to 3.8% of the global gross domestic product could be lost due to this problem. Methicillin-resistant <i>Staphylococcus aureus</i> is one of the leading sources of hospital-acquired infections associated with increased mortality, length of hospital stay, and higher cost of treatment. Here, we describe the de novo synthesis of a library of 22 triazeneindole derivatives with high activity against a wide panel of multidrug-resistant MRSA clinical isolates. Leading compound BX-SI043 (ethyl 6-fluoro-3-[pyrrolidin-1-yl-azo]-1H-indole-2-carboxylate) showed high activity (minimal inhibitory concentration range, 0.125-0"],"journal":["International journal of molecular sciences"],"pubmed_title":["Novel Triazeneindole Antibiotics: Synthesis and Hit-to-Lead Optimization."],"pmcid":["PMC11899342"],"funding_grant_id":["FSMG-2021-0006, \"Digital technologies for solving problems of quantitative medicine\", agree-ment 075-03-2024-117 dated 17 January 2024"],"pubmed_authors":["Gvozd A","Yampolsky I","Kublitski V","Shmygarev V","Filimonova A","Kuzmin D","Guglya E","Sorokin B","Emelianova A","Gusev E"],"additional_accession":[]},"is_claimable":false,"name":"Novel Triazeneindole Antibiotics: Synthesis and Hit-to-Lead Optimization.","description":"Bacterial antibiotic resistance represents a major healthcare problem. In 2019, 4.95 million deaths were associated with antibiotic resistance, and it is estimated that, by 2050, up to 3.8% of the global gross domestic product could be lost due to this problem. Methicillin-resistant <i>Staphylococcus aureus</i> is one of the leading sources of hospital-acquired infections associated with increased mortality, length of hospital stay, and higher cost of treatment. Here, we describe the de novo synthesis of a library of 22 triazeneindole derivatives with high activity against a wide panel of multidrug-resistant MRSA clinical isolates. Leading compound BX-SI043 (ethyl 6-fluoro-3-[pyrrolidin-1-yl-azo]-1H-indole-2-carboxylate) showed high activity (minimal inhibitory concentration range, 0.125-0","dates":{"release":"2025-01-01T00:00:00Z","publication":"2025 Feb","modification":"2025-04-04T09:07:56.739Z","creation":"2025-04-04T09:07:56.739Z"},"accession":"S-EPMC11899342","cross_references":{"pubmed":["40076499"],"doi":["10.3390/ijms26051870"]}}