Issue 44, 2015

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

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

Supplementary files

Article information

Article type
Paper
Submitted
15 Jul 2015
Accepted
08 Sep 2015
First published
08 Sep 2015

Org. Biomol. Chem., 2015,13, 10923-10928

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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