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.
AmpC beta-lactamase in complex with a p.carboxyphenylboronic acid / Tondi, Donatella. - ELETTRONICO. - (2009), pp. 1-1. [10.2210/pdb3bm6/pdb]
AmpC beta-lactamase in complex with a p.carboxyphenylboronic acid
TONDI, Donatella
2009
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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