RESUMO
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.
Assuntos
Antibacterianos/farmacologia , Bactérias/efeitos dos fármacos , Cetolídeos/farmacologia , Antibacterianos/química , Antibacterianos/farmacocinética , Farmacorresistência Bacteriana , Humanos , Cetolídeos/química , Cetolídeos/farmacocinética , Macrolídeos/química , Macrolídeos/farmacocinética , Macrolídeos/farmacologia , Patentes como AssuntoRESUMO
During the course of our investigations in the field of azole antimicrobial agents, we have identified BM 212, a pyrrole derivative with good in vitro activity against mycobacteria and candidae. These findings prompted us to prepare new pyrrole derivatives 1-10 in the hope of increasing the activity. The microbiological data showed interesting in vitro activity against Mycobacterium tuberculosis and atypical mycobacteria.
