Assessment of the rules related to gaining activity against Gram-negative bacteria.
Cast your vote
You can rate an item by clicking the amount of stars they wish to award to this item.
When enough users have cast their vote on this item, the average rating will also be shown.
Your vote was cast
Thank you for your feedback
Thank you for your feedback
Hirsch, Anna K H
MetadataShow full item record
AbstractIn 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 Escherichia coli wild-type K12, whereas more distinct activity differences were observed in E. coli mutant strains ΔtolC, D22, ΔacrB and BL21(DE3)omp8. A comparison of the activity results of the E. coli mutants with respect to the known rules related to enhanced activity against Gram-negative bacteria revealed that applicability of the rules is not always ensured. Out of the four amino acids used in this study, glycine derivatives showed highest antibacterial activity, although still suffering from efflux issues.
CitationRSC Med Chem. 2021 Mar 3;12(4):593-601. doi: 10.1039/d0md00409j.
AffiliationHIPS, Helmholtz-Institut für Pharmazeutische Forschung Saarland, Universitätscampus E8.1 66123 Saarbrücken, Germany.
PublisherRoyal Society of Chemistry
JournalRSC medicinal chemistry
The following license files are associated with this item:
- Creative Commons
- Facilitating Compound Entry as a Means to Discover Antibiotics for Gram-Negative Bacteria.
- Authors: Muñoz KA, Hergenrother PJ
- Issue date: 2021 Mar 16
- Functional characterization of a new holin-like antibacterial protein coding gene tmp1 from goat skin surface metagenome.
- Authors: Rajesh T, Anthony T, Saranya S, Pushpam PL, Gunasekaran P
- Issue date: 2011 Feb
- Progress against Escherichia coli with the Oxazolidinone Class of Antibacterials: Test Case for a General Approach To Improving Whole-Cell Gram-Negative Activity.
- Authors: Takrouri K, Cooper HD, Spaulding A, Zucchi P, Koleva B, Cleary DC, Tear W, Beuning PJ, Hirsch EB, Aggen JB
- Issue date: 2016 Jun 10
- [The history of the development and changes of quinolone antibacterial agents].
- Authors: Takahashi H, Hayakawa I, Akimoto T
- Issue date: 2003
- Synergy between Active Efflux and Outer Membrane Diffusion Defines Rules of Antibiotic Permeation into Gram-Negative Bacteria.
- Authors: Krishnamoorthy G, Leus IV, Weeks JW, Wolloscheck D, Rybenkov VV, Zgurskaya HI
- Issue date: 2017 Oct 31