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.
Structural study of phenyl boronic acid derivatives as AmpC beta-lactamase inhibitors / TONDI, Donatella; Calò, Samuele; Shoichet, BK; COSTI, Maria Paola. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - STAMPA. - 20:11(2010), pp. 3416-3419. [10.1016/j.bmcl.2010.04.007]
Structural study of phenyl boronic acid derivatives as AmpC beta-lactamase inhibitors
TONDI, Donatella
Investigation
;COSTI, Maria Paola
Visualization
2010
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.
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