Thiourea-based spacers in potent divalent inhibitors of Pseudomonas aeruginosa virulence lectin LecA
Publication date
2015-11-03
Authors
Pukin, Aliaksei
Brouwer, Arwin J
Koomen, Leonie
Quarles Van Ufford, H. C.
Kemmink, Johan
de Mol, N.J.
Pieters, Roland J.
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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.
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Citation
Pukin, A V, Brouwer, A J, Koomen, L, Quarles van Ufford, H C, Kemmink, J, de Mol, N J & Pieters, R J 2015, 'Thiourea-based spacers in potent divalent inhibitors of Pseudomonas aeruginosa virulence lectin LecA', Organic & Biomolecular Chemistry, vol. 13, no. 44, pp. 10923-10928. https://doi.org/10.1039/c5ob01452b