The remarkably broad spectrum of antimicrobial activity of the tetracyclines notwithstanding, the widespread emergence of bacterial genes and plasmids encoding tetracy-cline resistance has increasingly imposed limitations on the clinical applications of this antibiotic class in recent years.164 This situation has prompted researchers at Lederle Laboratories to reinvestigate SARs of tetracy-clines substituted in the aromatic (D) ring in an effort to discover analogs that might be effective against resistant strains. As a result of these efforts, the glycylcyclines, a class of 9-dimethylglycylamino-(DMG)-substituted tetracyclines exemplified by DMG-minocycline (DMG-MINO), and DMG-6-methyl-6-deoxytetracycline (DMG-DMDOT) were discovered.187-189
The first of these to be marketed was tigecycline.
The glycylcyclines retain the broad spectrum of activity and potency exhibited by the original tetracyclines against tetracycline-sensitive microbial strains and are highly active against bacterial strains that exhibit tetracycline resistance mediated by efflux or ribosomal protection determinants. If ongoing clinical evaluations of the glycylcyclines establish favorable toxicological and pharmacokinetic profiles for these compounds, a new class of "second-generation" tetra-cyclines could be launched.
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