PMID:16271472

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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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