PMID:16271472
| Citation |
Strancar, K, Blanot, D and Gobec, S (2006) Design, synthesis and structure-activity relationships of new phosphinate inhibitors of MurD. Bioorg. Med. Chem. Lett. 16:343-8 |
|---|---|
| Abstract |
A series of new phosphinate compounds were designed and synthesized as inhibitors of the d-glutamic acid-adding enzyme (MurD) involved in peptidoglycan biosynthesis. They were tested against the MurD enzyme from Escherichia coli, allowing initial structure-activity relationships to be deduced. Two compounds had IC(50) values near 100 microM and constitute a promising starting point for further development. |
| Links |
PubMed Online version:10.1016/j.bmcl.2005.09.086 |
| Keywords |
Bacterial Proteins/antagonists & inhibitors; Bacterial Proteins/metabolism; Drug Design; Enzyme Inhibitors/chemical synthesis; Enzyme Inhibitors/chemistry; Enzyme Inhibitors/pharmacology; Escherichia coli/enzymology; Molecular Structure; Peptide Synthases/antagonists & inhibitors; Peptide Synthases/metabolism; Peptidoglycan/biosynthesis; Peptidoglycan/drug effects; Phosphinic Acids/chemical synthesis; Phosphinic Acids/chemistry; Phosphinic Acids/pharmacology; Stereoisomerism; Structure-Activity Relationship |
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