omadacycline and Escherichia-coli-Infections

A novel series of fully synthetic 8-azatetracyclines was prepared and evaluated for antibacterial activity. Compounds were identified that overcome both efflux (tet(K)) and ribosomal protection (tet(M)) tetracycline resistance mechanisms and are active against Gram-positive and Gram-negative organisms. Two compounds were identified that exhibit comparable efficacy to marketed tetracyclines in in vivo models of bacterial infection.

Topics: Administration, Oral; Animals; Anti-Bacterial Agents; Aza Compounds; Biological Availability; Escherichia coli Infections; Gram-Negative Bacteria; Gram-Positive Bacteria; Injections, Intravenous; Mice; Microbial Sensitivity Tests; Rats; Rats, Sprague-Dawley; Sepsis; Streptococcal Infections; Structure-Activity Relationship; Tetracycline Resistance; Tetracyclines