title: Enoyl acyl carrier protein reductase inhibitors: an updated patent review (2011 - 2015).
abstract: BACKGROUND
  Enoyl-(acyl-carrier-protein) reductase (ENR) is a limiting step enzyme in the Fatty Acid Synthase II system. In mammals, there is no homologue to ENR, which makes it an optimal candidate target for selective anti-infective drugs. Up-to-date, only two ENR inhibitors are used in clinical practice.
  
  
  METHODS
  This review is a survey on important patents on low molecular weight compounds with ENR inhibiting activity published in 2011-2015. Common patent databases (SciFinder, esp@cenet, WIPO) were used to locate patent applications on the proposed topic and in the timespan of 2011-2015.
  
  
  CONCLUSIONS
  In 2011-2015, we have observed patents in previously known structural groups of diphenyl ethers and acrylamides as well as new structural classes, often identified by high-throughput screening campaigns. The spectrum of activity of applied derivatives covers significant bacteria, mycobacteria, and apicomplexan parasites (Plasmodia and Toxoplasma). Good news from research of ENR inhibitors: a) four selective anti-staphylococcal compounds applied in 2011-2015 or earlier were pushed to Phase I or Phase II clinical trials and some of them proved safety and tolerability after peroral and/or intravenous administration; b) big pharma companies have renewed their interest in the development of new anti-infective compounds against resistant strains of clinical relevance.
authors.affiliation: a Department of Pharmaceutical Chemistry and Pharmaceutical Analysis, Faculty of Pharmacy in Hradec Králové , Charles University in Prague , Hradec Králové , Czech Republic.
authors.forename: Jan
authors.initials: J
authors.lastname: Zitko
authors.affiliation: a Department of Pharmaceutical Chemistry and Pharmaceutical Analysis, Faculty of Pharmacy in Hradec Králové , Charles University in Prague , Hradec Králové , Czech Republic.
authors.forename: Martin
authors.initials: M
authors.lastname: Doležal
mesh_terms: D000818:Animals; D000890:Anti-Infective Agents / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use; D015195:Drug Design; D004352:Drug Resistance, Microbial; D050753:Enoyl-(Acyl-Carrier-Protein) Reductase (NADH) / Q000037:antagonists & inhibitors* / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use; D057166:High-Throughput Screening Assays; D006801:Humans; D010330:Patents as Topic
chemical_list: D000890:Anti-Infective Agents; D004791:Enzyme Inhibitors; D050753:Enoyl-(Acyl-Carrier-Protein) Reductase (NADH)
keywords: Acrylamide; FabI; InhA; MRSA; antibacterial; antimycobacterial; enoyl-acyl-carrier-protein reductase; triclosan