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  • Title: C-9 Alkenylidine bridged macrolides: WO2008061189. Enanta Pharmaceuticals, Inc.
    Author: Poce G, Cesare Porretta G, Biava M.
    Journal: Expert Opin Ther Pat; 2009 Jun; 19(6):901-6. PubMed ID: 19473109.
    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.
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