Synthesis and evaluation of boronic acids as inhibitors of Penicillin Binding Proteins of classes A, B and C

Astrid Zervosen, André Bouillez, Alexandre Herman, Ana Amoroso, Bernard Joris, Eric Sauvage, Paulette Charlier, André Luxen, Astrid Zervosen, André Bouillez, Alexandre Herman, Ana Amoroso, Bernard Joris, Eric Sauvage, Paulette Charlier, André Luxen

Index: Bioorg. Med. Chem. 20(12) , 3915-24, (2012)

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Abstract

After the identification of (2,6-dimethoxybenzamido)methylboronic acid as a potent inhibitor of R39 from Actinomadura (IC50: 1.3μM) various acylaminomethylboronic acids were synthesized. (2-Nitrobenzamido)methylboronic acid inhibits Penicillin Binding Proteins of classes A, B and C.