Substrate‐Inspired Fragment Merging and Growing Affords Efficacious LasB Inhibitors

Extracellular virulence factors have emerged as attractive targets in the current antimicrobial resistance crisis. The Gram‐negative pathogen Pseudomonas aeruginosa secretes the virulence factor elastase B (LasB), which plays an important role in the infection process. Here, we report a sub‐micromol...

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Veröffentlicht in:	Angewandte Chemie International Edition 2022-01, Vol.61 (5), p.e202112295-n/a
Hauptverfasser:	Kaya, Cansu, Walter, Isabell, Yahiaoui, Samir, Sikandar, Asfandyar, Alhayek, Alaa, Konstantinović, Jelena, Kany, Andreas M., Haupenthal, Jörg, Köhnke, Jesko, Hartmann, Rolf W., Hirsch, Anna K. H.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Anti-Bacterial Agents - chemical synthesis Anti-Bacterial Agents - chemistry Anti-Bacterial Agents - pharmacology Antibiotic resistance Antimicrobial resistance Antivirulence Bacterial Proteins - antagonists & inhibitors Bacterial Proteins - chemistry Bacterial Proteins - metabolism Communication Communications Crystal structure Drug development Elastase Fragment merging Inhibitors Inspection Larva - drug effects Larvae Mercaptoacetamides Microbial Sensitivity Tests Models, Molecular Molecular Structure Moths Pancreatic Elastase - antagonists & inhibitors Pancreatic Elastase - metabolism Pseudomonas aeruginosa Pseudomonas aeruginosa - drug effects Selectivity Structure-Activity Relationship Substrates Virulence Virulence factors
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