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Structural study of phenyl boronic acid derivatives as AmpC beta-lactamase inhibitors.

ABSTRACT: A small set of boronic acids acting as low nanomolar inhibitors of AmpC beta-lactamase were designed and synthesized in the effort to improve affinity, pharmacokinetic properties, and to provide a valid lead compound. X-ray crystallography revealed the binary complex of the best inhibitor bound to the enzyme, highlighting possibilities for its further rational derivatization and chemical optimization.

SUBMITTER: Tondi D 

PROVIDER: S-EPMC3177945 | biostudies-literature | 2010 Jun

REPOSITORIES: biostudies-literature

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Structural study of phenyl boronic acid derivatives as AmpC beta-lactamase inhibitors.

Tondi Donatella D   Calò Samuele S   Shoichet Brian K BK   Costi Maria Paola MP  

Bioorganic & medicinal chemistry letters 20100409 11

A small set of boronic acids acting as low nanomolar inhibitors of AmpC beta-lactamase were designed and synthesized in the effort to improve affinity, pharmacokinetic properties, and to provide a valid lead compound. X-ray crystallography revealed the binary complex of the best inhibitor bound to the enzyme, highlighting possibilities for its further rational derivatization and chemical optimization. ...[more]

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