GLYCYLCYCLINES .1. A NEW-GENERATION OF POTENT ANTIBACTERIAL AGENTS THROUGH MODIFICATION OF 9-AMINOTETRACYCLINES

This report describes the discovery of a new generation of tetracycline antibacterial agents, the ''glycylcyclines''. These agents are notable for their activity against a broad spectrum of tetracycline-susceptible and -resistant Gram-negative and Gram-positive aerobic and anaerobic bacteria possessing various classes of tetracycline-resistant determinants [tet B (efflux), tet M (ribosomal protection)]. The design and synthesis of a number of 7-substituted 9-substituted-amido 6-demethyl-6-deoxytetracyclines are described.