2-Nitrobenzyl Esters of Penam and Cephem Derivatives as Inhibitors of Penicillin-Binding Proteins
(2013) Asian Journal of Organic Chemistry — Vol. 2, n° 8, p. 654-661 (2013)
Files
No attached file found for this publication.
Details
- Authors
- Abstract
- Nitroveratrole esters (i.e. 4,5-dimethoxy-2-nitrobenzyl (NV) esters) of penicillin and cephalosporin derivatives have been prepared in the course of a program dedicated to photosensitive protein microarrays. Surprisingly, some molecules revealed to be acylating inhibitors of R39 and BlaR-CTD proteins (two representative Penicillin Binding Proteins (PBPs)), while being bad substrates of beta-lactamases (bacterial defense enzymes). Electrostatic potential maps and docking experiments showed that the 2-nitro group of NV esters could play the role of a carboxylate in the penam series.
- Affiliations
Uliège Centre d’Ingénierie des Protéines (CIP)
Citations
Brulé, C., Grugier, J., Brans, A., Joris, B., Sauvage, E., Dive, G., & Marchand-Brynaert, J. (2013). 2-Nitrobenzyl Esters of Penam and Cephem Derivatives as Inhibitors of Penicillin-Binding Proteins. Asian Journal of Organic Chemistry, 2(8), 654-661. https://doi.org/10.1002/ajoc.201300108 (Original work published 2013)