tylosin and rosaramicin

Reductive amination of repromicin with polyfunctional amines has led to new macrolide antibacterial agents, some of which are highly potent against the Gram-negative pathogen Pasteurella multocida both in vitro and in a mouse infection model. A key element in this discovery was the recognition that among certain known macrolides increasing lipophilicity results in diminished in vivo activity. One repromicin derivative, 20-[N-[3-(dimethylamino)-propyl]-N-L-alanylamino]-20-deoxorepro micin (35), was selected for advanced evaluation. At 5 mg/kg, a single subcutaneous dose was found to control induced pasteurellosis in swine and induced respiratory disease in cattle.

Topics: Animals; Anti-Bacterial Agents; Chromatography, High Pressure Liquid; Leucomycins; Macrolides; Mice; Microbial Sensitivity Tests; Molecular Structure; Pasteurella Infections; Pasteurella multocida; Tylosin