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Bioorg Med Chem Lett. 2009 Nov 15;19(22):6350-2. doi: 10.1016/j.bmcl.2009.09.077. Epub 2009 Sep 24.

Inhibitors of bacterial N-succinyl-L,L-diaminopimelic acid desuccinylase (DapE) and demonstration of in vitro antimicrobial activity.

Author information

1
Department of Chemistry, Loyola University, 6525 North Sheridan Road, Chicago, IL 60626, USA.

Abstract

The dapE-encoded N-succinyl-L,L-diaminopimelic acid desuccinylase (DapE) is a critical bacterial enzyme for the construction of the bacterial cell wall. A screen biased toward compounds containing zinc-binding groups (ZBG's) including thiols, carboxylic acids, boronic acids, phosphonates and hydroxamates has delivered a number of micromolar inhibitors of DapE from Haemophilus influenzae, including the low micromolar inhibitor L-captopril (IC(50)=3.3 microM, K(i)=1.8 microM). In vitro antimicrobial activity was demonstrated for L-captopril against Escherichia coli.

PMID:
19822427
DOI:
10.1016/j.bmcl.2009.09.077
[Indexed for MEDLINE]

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