{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Ropponen HK"],"funding":["Helmholtz Association","Verband der Chemischen Industrie"],"pagination":["593-601"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC8128065"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["12(4)"],"pubmed_abstract":["In the search for new antibacterial compounds, we repositioned an antimalarial compound class by derivatising it based on the so-called \"eNTRy\" rules for enhanced accumulation into Gram-negative bacteria. We designed, synthesised and evaluated a small library of amino acid modified compounds together with the respective Boc-protected analogues, leading to no substantial improvement in antibacterial activity against <i>Escherichia coli</i> wild-type K12, whereas more distinct activity differences were observed in <i>E. coli</i> mutant strains Δ<i>tolC</i>, D22, Δ<i>acrB</i> and BL21(DE3)omp8. A comparison of the activity results of the <i>E. coli</i> mutants with respect to the known rules related to enhanced activity against Gram-negative bacteria revealed that applicability of the rules i"],"journal":["RSC medicinal chemistry"],"pubmed_title":["Assessment of the rules related to gaining activity against Gram-negative bacteria."],"pmcid":["PMC8128065"],"funding_grant_id":["Kekulé Mobility Fellowship","Initiative and Networking Fund"],"pubmed_authors":["Hirsch AKH","Ropponen HK","Rottmann M","Fischer M","Illarionov B","Haupenthal J","Siemens A","Witschel M","Diamanti E"],"additional_accession":[]},"is_claimable":false,"name":"Assessment of the rules related to gaining activity against Gram-negative bacteria.","description":"In the search for new antibacterial compounds, we repositioned an antimalarial compound class by derivatising it based on the so-called \"eNTRy\" rules for enhanced accumulation into Gram-negative bacteria. We designed, synthesised and evaluated a small library of amino acid modified compounds together with the respective Boc-protected analogues, leading to no substantial improvement in antibacterial activity against <i>Escherichia coli</i> wild-type K12, whereas more distinct activity differences were observed in <i>E. coli</i> mutant strains Δ<i>tolC</i>, D22, Δ<i>acrB</i> and BL21(DE3)omp8. A comparison of the activity results of the <i>E. coli</i> mutants with respect to the known rules related to enhanced activity against Gram-negative bacteria revealed that applicability of the rules i","dates":{"release":"2021-01-01T00:00:00Z","publication":"2021 Apr","modification":"2025-05-29T21:23:42.124Z","creation":"2025-05-29T21:23:42.124Z"},"accession":"S-EPMC8128065","cross_references":{"pubmed":["34046630"],"doi":["10.1039/d0md00409j"]}}