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Discovery of VNRX-7145 (VNRX-5236 Etzadroxil): An Orally Bioavailable β-Lactamase Inhibitor for Enterobacterales Expressing Ambler Class A, C, and D Enzymes

Robert E. Lee Trout, Allison L. Zulli, Eugen F. Mesaros, Randy W. Jackson, Steven A. Boyd, Bin Liu, Jodie C. Hamrick, Denis M. Daigle, Cassandra L. Chatwin, Kaitlyn John, Lisa McLaughlin, Susan M. Cusick, Jason Weiss, Mark Pulse, Daniel C. Pevear, Greg Moeck, L Xerri, Christopher J. Burns

2021Journal of Medicinal Chemistry47 citationsDOIOpen Access PDF

Abstract

restored the activity of the oral cephalosporin antibiotic ceftibuten against Enterobacterales expressing Ambler class A extended-spectrum β-lactamases, class A carbapenemases, class C cephalosporinases, and class D oxacillinases.

Topics & Concepts

ProdrugBioavailabilityChemistryAntibioticsAntimicrobialPharmacokineticsPharmacologyCephalosporinIn vivoMeropenemAntibiotic resistanceBiochemistryMedicineBiologyBiotechnologyOrganic chemistryAntibiotic Resistance in BacteriaAntibiotic Use and ResistanceAntibiotics Pharmacokinetics and Efficacy
Discovery of VNRX-7145 (VNRX-5236 Etzadroxil): An Orally Bioavailable β-Lactamase Inhibitor for Enterobacterales Expressing Ambler Class A, C, and D Enzymes | Litcius