title: C-9 Alkenylidine bridged macrolides: WO2008061189. Enanta Pharmaceuticals, Inc.
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.
authors.affiliation: Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza University of Rome, Piazzale A. Moro 5, I 00185 Rome, Italy. giovanna.poce@uniroma1.it
authors.forename: Giovanna
authors.initials: G
authors.lastname: Poce
authors.forename: Giulio
authors.initials: G
authors.lastname: Cesare Porretta
authors.forename: Mariangela
authors.initials: M
authors.lastname: Biava
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects*; D024881:Drug Resistance, Bacterial; D006801:Humans; D048628:Ketolides / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D018942:Macrolides / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D010330:Patents as Topic
chemical_list: D000900:Anti-Bacterial Agents; D048628:Ketolides; D018942:Macrolides