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Bioorg Med Chem Lett. 2006 Jan 15;16(2):343-8. Epub 2005 Nov 3.

Design, synthesis and structure-activity relationships of new phosphinate inhibitors of MurD.

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1
University of Ljubljana, Faculty of Pharmacy, Askerceva 7, 1000 Ljubljana, Slovenia.

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.

PMID:
16271472
DOI:
10.1016/j.bmcl.2005.09.086
[Indexed for MEDLINE]
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