ArticleJournal of medicinal chemistry2022
LEGO-Lipophosphonoxins: A Novel Approach in Designing Membrane Targeting Antimicrobials.
Article in Journal of medicinal chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.
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Who cites it
6 citing papers in PubMed.
- Biological profiling of structurally diverse LEGO-LPPOs reveals differences in antibacterial activity, cytocompatibility, and in vivo tolerability.The Journal of antibiotics · 2026Article
- LEGO-Lipophosphonoxin membrane activity is enhanced by presence of phosphatidylethanolamine but hindered by outer membrane.Scientific reports · 2025Article
- Assessment ofBiomolecules · 2024Article
- LEGO-lipophosphonoxins: length of hydrophobic module affects permeabilizing activity in target membranes of different phospholipid composition.RSC advances · 2024Article
- Lipophosphonoxins-A Novel Group of Broad Spectrum Antibacterial Compounds.Pharmaceutics · 2023Review
- Synthesis and Biological Evaluation of Piperazine Hybridized Coumarin Indolylcyanoenones with Antibacterial Potential.Molecules (Basel, Switzerland) · 2023Article
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Authors and funding
20 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The alarming rise of bacterial antibiotic resistance requires the development of new compounds. Such compounds, lipophosphonoxins (LPPOs), were previously reported to be active against numerous bacterial species, but serum albumins abolished their activity. Here we describe the synthesis and evaluation of novel antibacterial compounds termed LEGO-LPPOs, loosely based on LPPOs, consisting of a central linker module with two attached connector modules on either side. The connector modules are then decorated with polar and hydrophobic modules. We performed an extensive structure-activity relationship study by varying the length of the linker and hydrophobic modules. The best compounds were active against both Gram-negative and Gram-positive species including multiresistant strains and persisters. LEGO-LPPOs act by first depleting the membrane potential and then creating pores in the cytoplasmic membrane. Importantly, their efficacy is not affected by the presence of serum albumins. Low cytotoxicity and low propensity for resistance development demonstrate their potential for therapeutic use.
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Registered trials
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