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
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.