Back to Search
Start Over
1,3-Phenylene bis(ketoacid) derivatives as inhibitors of Escherichia coli dihydrodipicolinate synthase.
- Source :
-
Bioorganic & medicinal chemistry [Bioorg Med Chem] 2012 Apr 01; Vol. 20 (7), pp. 2419-26. Date of Electronic Publication: 2012 Feb 10. - Publication Year :
- 2012
-
Abstract
- Dihydrodipicolinate synthase is a key enzyme in the lysine biosynthesis pathway that catalyzes the condensation of pyruvate and aspartate semi-aldehyde. A series of phenolic ketoacid derivatives that mimic the proposed enzymatic intermediate were designed as potential inhibitors of this enzyme and were synthesized from simple precursors. The ketoacid derivatives were shown to act as slow and slow-tight binding inhibitors. Mass spectrometric experiments provided further evidence to support the proposed model of inhibition, demonstrating either an encounter complex or a condensation product for the slow and slow-tight binding inhibitors, respectively.<br /> (Copyright © 2012 Elsevier Ltd. All rights reserved.)
- Subjects :
- Enzyme Inhibitors chemical synthesis
Escherichia coli Proteins metabolism
Hydro-Lyases metabolism
Keto Acids chemical synthesis
Kinetics
Mass Spectrometry
Enzyme Inhibitors chemistry
Escherichia coli enzymology
Escherichia coli Proteins antagonists & inhibitors
Hydro-Lyases antagonists & inhibitors
Keto Acids chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3391
- Volume :
- 20
- Issue :
- 7
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 22386717
- Full Text :
- https://doi.org/10.1016/j.bmc.2012.01.045