We thank the Canadian Institutes for Health Research (CIHR) for funding to S.G.W. and the BBSRC for funding to G.J.D. E.J.T. is a Royal Society University Research Fellow, and G.J.D. is a Royal Society/Wolfson Research Merit Award recipient.
Chitinase Inhibition by Chitobiose and Chitotriose Thiazolines†
Article first published online: 5 MAR 2010
Copyright © 2010 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
Angewandte Chemie International Edition
Volume 49, Issue 14, pages 2599–2602, March 29, 2010
How to Cite
Macdonald, James M., Tarling, Chris A., Taylor, Edward J., Dennis, Rebecca J., Myers, David S., Knapp, S., Davies, Gideon J. and Withers, Stephen G. (2010), Chitinase Inhibition by Chitobiose and Chitotriose Thiazolines. Angew. Chem. Int. Ed., 49: 2599–2602. doi: 10.1002/anie.200906644
- Issue published online: 23 MAR 2010
- Article first published online: 5 MAR 2010
- Manuscript Received: 25 NOV 2009
- Canadian Institutes for Health Research (CIHR)
- enzyme inhibitors;
A good imitation: Di- and trisaccharide analogues of the oxazoline intermediate formed during enzymatic hydrolysis of chitin were found to be potent inhibitors of chitinase A. The high affinity and enzymatic stability of a readily synthesized thioamide trisaccharide (two molecules of which are shown in the enzyme active site), and the mechanism-based mode of inhibition, make this analogue a promising candidate for broad-spectrum chitinase inhibition.