C-9 Alkenylidine bridged macrolides: WO2008061189. Enanta Pharmaceuticals, Inc

Expert Opin Ther Pat. 2009 Jun;19(6):901-6. doi: 10.1517/13543770902762901.

Abstract

Ketolides, which represent the third generation of erythromycin A derivatives, were developed as a result of the need for new and potent antibacterial agents. This class of compounds has a significantly improved pharmacokinetic profile and, above all, shows activity against macrolide-resistant strains. When compared with other macrolides, ketolide structural differences are characterized by the removal of the 3-O-cladinose moiety and by a heteroaryl-alkyl side chain attached to the macrocycle by a flexible linker. The bridged bicyclic ketolides (BBK) are one of the three classes of ketolide; the present application from Enanta Pharmaceuticals, Inc. discloses a series of novel C-9 alkenylidine bridged macrolides belonging to BBK. These compounds are 3,6- and 6,11-bicyclolides, which have the alkenylidine second anchor portion attached to C-9 of the molecule.

Publication types

  • Comparative Study

MeSH terms

  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacokinetics
  • Anti-Bacterial Agents / pharmacology*
  • Bacteria / drug effects*
  • Drug Resistance, Bacterial
  • Humans
  • Ketolides / chemistry
  • Ketolides / pharmacokinetics
  • Ketolides / pharmacology*
  • Macrolides / chemistry
  • Macrolides / pharmacokinetics
  • Macrolides / pharmacology
  • Patents as Topic

Substances

  • Anti-Bacterial Agents
  • Ketolides
  • Macrolides