1. Thiourea-based spacers in potent divalent inhibitors of Pseudomonas aeruginosa virulence lectin LecA.
- Author
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Pukin AV, Brouwer AJ, Koomen L, Quarles van Ufford HC, Kemmink J, de Mol NJ, and Pieters RJ
- Subjects
- Humans, Lectins antagonists & inhibitors, Lectins metabolism, Molecular Docking Simulation, Pseudomonas Infections drug therapy, Pseudomonas Infections microbiology, Pseudomonas aeruginosa pathogenicity, Virulence Factors antagonists & inhibitors, Adhesins, Bacterial metabolism, Anti-Bacterial Agents chemistry, Anti-Bacterial Agents pharmacology, Pseudomonas aeruginosa drug effects, Thiourea analogs & derivatives, Thiourea pharmacology, Virulence Factors metabolism
- Abstract
A new divalent highly potent inhibitor of the Pseudomonas aeruginosa lectin and virulence factor LecA was prepared. It contains two thiourea linkages which were found to be in the Z,Z isomeric form. This brings the spacer into an elongated conformation required to bridge the two binding sites, which results in the chelating binding mode responsible for the high potency.
- Published
- 2015
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