Document Detail

Inhibitors of bacterial N-succinyl-L,L-diaminopimelic acid desuccinylase (DapE) and demonstration of in vitro antimicrobial activity.
MedLine Citation:
PMID:  19822427     Owner:  NLM     Status:  MEDLINE    
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.
Danuta Gillner; Nicola Armoush; Richard C Holz; Daniel P Becker
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Publication Detail:
Type:  Journal Article; Research Support, U.S. Gov't, Non-P.H.S.     Date:  2009-09-24
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  19     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2009 Nov 
Date Detail:
Created Date:  2009-10-26     Completed Date:  2010-01-27     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  6350-2     Citation Subset:  IM    
Department of Chemistry, Loyola University, 6525 North Sheridan Road, Chicago, IL 60626, USA.
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MeSH Terms
Amidohydrolases / antagonists & inhibitors*,  metabolism
Amino Acid Sequence
Anti-Bacterial Agents / pharmacology*
Binding Sites
Diaminopimelic Acid / metabolism*
Enzyme Inhibitors / pharmacology*
Escherichia coli / drug effects*,  enzymology
Haemophilus influenzae / drug effects*,  enzymology
Microbial Sensitivity Tests
Mutagenesis, Site-Directed
Substrate Specificity
Reg. No./Substance:
0/Anti-Bacterial Agents; 0/Enzyme Inhibitors; 583-93-7/Diaminopimelic Acid; EC 3.5.-/Amidohydrolases

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