title: Oxazolidinone antimicrobials: a patent review (2012-2015).
abstract: BACKGROUND
  Antimicrobial resistance in Gram-positive bacteria is a major health care issue. This review summarizes patent publications from 2012 to 2015 that divulged novel oxazolidinones as antibacterial agents.
  
  
  METHODS
  A total of 25 patents obtained from Espacenet, WIPO Patentscope and FreePatentsOnline, and AcclaimIP search engines were reviewed. The patents were scrutinized based on the novelty of the compounds, their antibacterial activity (MIC, µg/mL), and the process of preparation. The oxazolidinones with promising antibacterial activity were classified according to the following structural diversities, as biaryl heterocyclic, fused heteroaryl rings containing oxazolidinones, and others. The biaryl heterocyclic, fused heteroaryl, benzoxazine, and the 1H-pyrazol-1-yl containing oxazolidinone derivatives demonstrated potent antibacterial activities superior to linezolid against Gram-positive bacteria. Some derivatives were effective against standard strains of Gram-negative bacteria, namely Moraxella catarrhalis ATCC A894, and Escherichia coli ATCC 25922. In addition, a patent disclosed a structural isomer of linezolid with marginal activity against the aerobic Gram-negative bacteria MDR Stenotrophomonas (Xanthomonas) maltophilia, while linezolid and vancomycin did not inhibit growth. Finally, some derivatives showed activity against respiratory infectious diseases' causative agents, such as B. anthracis, B. mallei, Y. pestis, and M. pneumoniae.
  
  
  CONCLUSIONS
  Overall, there is limited in vivo data to support the potential clinical advancement of the currently reported novel derivatives.
authors.affiliation: a Department of Pharmaceutical Chemistry, Faculty of Pharmacy , Kuwait University , Safat , Kuwait.
authors.forename: Oludotun A
authors.initials: OA
authors.lastname: Phillips
authors.affiliation: a Department of Pharmaceutical Chemistry, Faculty of Pharmacy , Kuwait University , Safat , Kuwait.
authors.forename: Leyla H
authors.initials: LH
authors.lastname: Sharaf
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D015195:Drug Design; D024901:Drug Resistance, Multiple, Bacterial; D006090:Gram-Negative Bacteria / Q000187:drug effects; D016905:Gram-Negative Bacterial Infections / Q000188:drug therapy; D006094:Gram-Positive Bacteria / Q000187:drug effects; D016908:Gram-Positive Bacterial Infections / Q000188:drug therapy; D006801:Humans; D008826:Microbial Sensitivity Tests; D023303:Oxazolidinones / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D010330:Patents as Topic
chemical_list: D000900:Anti-Bacterial Agents; D023303:Oxazolidinones
keywords: Antibacterial agents; Gram-negative bacteria; Gram-positive bacteria; antimicrobials; bacterial-resistance; fluoroquinolone-oxazolidinone hybrids; linezolid; oxazolidinone; tedizolid