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Phosphinate Inhibitors of UDP-N-Acetylmuramoyl-L-Alanyl-D-Glutamate: L-Lysine Ligase (MurE)

✍ Scribed by Katja Štrancar; Audrey Boniface; Didier Blanot; Stanislav Gobec

Publisher: John Wiley and Sons
Year: 2007
Tongue: English
Weight: 834 KB
Volume: 340
Category: Article
ISSN: 0365-6233
DOI: 10.1002/ardp.200600191

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✦ Synopsis

Abstract

The increasing emergence of pathogenic bacterial strains with high resistance to antibiotic therapy has created an urgent need for the development of new antibacterial agents that are directed towards novel targets. We have focused our attention on the Mur ligases (MurC‐F), which catalyze the early steps of bacterial peptidoglycan biosynthesis, and which to date represent under‐exploited targets for antibacterial drug design. We show that some of our phosphinate inhibitors of UDP‐N‐acetylmuramoyl‐L‐alanyl:D‐glutamate ligase (MurD) also inhibits UDP‐N‐acetylmuramoyl‐L‐alanyl‐D‐glutamate:L‐lysine ligase (MurE). To obtain new information on their structure‐activity relationships, three new, structurally related phosphinates were synthesized and evaluated for inhibition of MurD and MurE.

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