{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Dutta S"],"funding":["National Institute of Allergy and Infectious Diseases","University of Colorado Boulder","NIAID NIH HHS","National Institutes of Health"],"pagination":["128878"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC10101151"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["72"],"pubmed_abstract":["Multidrug-resistant (MDR) Gram-negative bacteria are an urgent and rapidly spreading threat to human health with limited treatment options. Previously, we discovered a novel [1,2,5]oxadiazolo[3,4-b]pyrazine-containing compound (1) that selectively re-sensitized a variety of MDR Gram-negative bacteria to colistin, one of the last-resort antibiotic. Herein, we report the structure-activity relationship studies of compound 1 that led to the discovery of several more potent and/or less toxic resistance-modifying agents (RMAs). Further evaluation of these RMAs showed that they were effective in a wide range of MDR bacteria. These results demonstrated these compounds as a novel class of RMAs and may be further developed as therapeutic agents."],"journal":["Bioorganic & medicinal chemistry letters"],"pubmed_title":["Structure-activity relationship studies of [1,2,5]oxadiazolo[3,4-b]pyrazine-containing polymyxin-selective resistance-modifying agents."],"pmcid":["PMC10101151"],"funding_grant_id":["R33AI121581","R33 AI121581"],"pubmed_authors":["Dutta S","Liu N","Gao Y","Beck L","Wang X"],"additional_accession":[]},"is_claimable":false,"name":"Structure-activity relationship studies of [1,2,5]oxadiazolo[3,4-b]pyrazine-containing polymyxin-selective resistance-modifying agents.","description":"Multidrug-resistant (MDR) Gram-negative bacteria are an urgent and rapidly spreading threat to human health with limited treatment options. Previously, we discovered a novel [1,2,5]oxadiazolo[3,4-b]pyrazine-containing compound (1) that selectively re-sensitized a variety of MDR Gram-negative bacteria to colistin, one of the last-resort antibiotic. Herein, we report the structure-activity relationship studies of compound 1 that led to the discovery of several more potent and/or less toxic resistance-modifying agents (RMAs). Further evaluation of these RMAs showed that they were effective in a wide range of MDR bacteria. These results demonstrated these compounds as a novel class of RMAs and may be further developed as therapeutic agents.","dates":{"release":"2022-01-01T00:00:00Z","publication":"2022 Sep","modification":"2025-04-19T23:48:01.813Z","creation":"2025-04-19T23:48:01.813Z"},"accession":"S-EPMC10101151","cross_references":{"pubmed":["35788034"],"doi":["10.1016/j.bmcl.2022.128878"]}}