title: Diazabicyclooctanes (DBOs): a potent new class of non-β-lactam β-lactamase inhibitors.
abstract: The β-lactams have been among the most successful classes of antibacterial agents for the past half century. However, a disturbing increase in resistance to β-lactams has been noted among Gram-negative bacteria, which is attributable to β-lactamase enzymes not within the spectrum of currently marketed β-lactams or β-lactam/β-lactamase inhibitor combinations. Diazabicyclooctanes (DBOs) were first investigated as β-lactam mimics in the mid-1990s by chemists at Hoechst Marion Roussel (now part of Sanofi-Aventis) and proved to be a rich source of β-lactamase inhibitors (BLI). Two members of this novel series of highly potent, broad spectrum BLIs are now in clinical development and their properties are reviewed here.
authors.affiliation: Arietis Corp, Boston, MA 02118, United States. k.coleman@arietiscorp.com
authors.forename: Ken
authors.initials: K
authors.lastname: Coleman
mesh_terms: D000900:Anti-Bacterial Agents / Q000494:pharmacology; D053961:Azabicyclo Compounds / Q000378:metabolism*; D001419:Bacteria / Q000187:drug effects / Q000201:enzymology*; D001424:Bacterial Infections / Q000188:drug therapy / Q000382:microbiology; D002986:Clinical Trials as Topic; D055808:Drug Discovery; D004791:Enzyme Inhibitors / Q000378:metabolism*; D006801:Humans; D065093:beta-Lactamase Inhibitors; D047090:beta-Lactams / Q000494:pharmacology
chemical_list: D000900:Anti-Bacterial Agents; D053961:Azabicyclo Compounds; D004791:Enzyme Inhibitors; D065093:beta-Lactamase Inhibitors; D047090:beta-Lactams