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Issue 44, 2015
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Thiourea-based spacers in potent divalent inhibitors of Pseudomonas aeruginosa virulence lectin LecA

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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.

Graphical abstract: Thiourea-based spacers in potent divalent inhibitors of Pseudomonas aeruginosa virulence lectin LecA

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Supplementary files

Article information


Submitted
15 Jul 2015
Accepted
08 Sep 2015
First published
08 Sep 2015

Org. Biomol. Chem., 2015,13, 10923-10928
Article type
Paper
Author version available

Thiourea-based spacers in potent divalent inhibitors of Pseudomonas aeruginosa virulence lectin LecA

A. V. Pukin, A. J. Brouwer, L. Koomen, H. C. Quarles van Ufford, J. Kemmink, N. J. de Mol and R. J. Pieters, Org. Biomol. Chem., 2015, 13, 10923
DOI: 10.1039/C5OB01452B

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