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Inhibitors of Bacterial N-Succinyl-L,L-diaminopimelic Acid Desuccinylase (DapE) and Demonstration of In Vitro Antimicrobial Activity
Bioorganic & Medicinal Chemistry Letters
  • Danuta Gillner
  • Nicola Armoush
  • Richard C. Holz
  • Daniel P. Becker, Loyola University Chicago
Document Type
Article
Publication Date
11-15-2009
Pages
6350-6352
Publisher Name
Elsevier
Disciplines
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 (IC50 = 3.3 μM, Ki = 1.8 μM). In vitro antimicrobial activity was demonstrated for l-captopril against Escherichia coli.

Comments

Author Posting © Elsevier, 2009. This is the author's version of the work. It is posted here by permission of Elsevier for personal use, not for redistribution. The definitive version was published in Bioorganic & Medicinal Chemistry Letters , Volume 19, Issue 22, November 15, 2009. http://dx.doi.org/10.1016/j.bmcl.2009.09.077

Creative Commons License
Creative Commons Attribution-Noncommercial-No Derivative Works 3.0
Citation Information
Danuta Gillner, Nicola Armoush, Richard C. Holz and Daniel P. Becker. "Inhibitors of Bacterial N-Succinyl-L,L-diaminopimelic Acid Desuccinylase (DapE) and Demonstration of In Vitro Antimicrobial Activity" Bioorganic & Medicinal Chemistry Letters Vol. 19 Iss. 12 (2009)
Available at: http://works.bepress.com/richard_holz/100/