molecules of the month


serine and metallo-beta-lactamase inhibitor

oral activity in resistant infection model

from optimization of literature starting point

J. Med. Chem., Apr. 2, 2020

Qpex Biopharma, San Diego, CA

1 min read

QPX7728 is an ultrabroad-spectrum beta-lactamase inhibitor with activity against both serine and zinc metallo-beta-lactamases, in contrast to approved beta-lactamase inhibitors such as relebactam which are only active against serine metalloproteases. Interestingly, the boron of the molecule coordinates to serine hydroxyl groups in serine beta-lactamases, whereas it coordinates as a boronate ligand to the zinc centers of metallo-beta-lactamases.

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