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

@article{Gillner2009InhibitorsOB,
  title={Inhibitors of bacterial N-succinyl-L,L-diaminopimelic acid desuccinylase (DapE) and demonstration of in vitro antimicrobial activity.},
  author={Danuta M. Gillner and Nicola Armoush and Richard C Holz and Daniel P Becker},
  journal={Bioorganic & medicinal chemistry letters},
  year={2009},
  volume={19 22},
  pages={
          6350-2
        }
}
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… CONTINUE READING
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Abstracts of Papers, 237th ACS National Meeting, Salt Lake City, UT

  • R. C. Holz, D. Gillner, D. Becker
  • United States, March 22-26,
  • 2009
1 Excerpt

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