| Autor: |
McFarland, J. W., Hecker, S. J., Jaynes, B. H., Jefson, M. R., Lundy, K. M., Vu, C. B., Glazer, E. A., Froshauer, S. A., Hayashi, S. F., Kamicker, B. J., Reese, C. P., Olson, J. A. |
| Zdroj: |
Journal of Medicinal Chemistry; March 14, 1997, Vol. 40 Issue: 6 p1041-1045, 5p |
| Abstrakt: |
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-deoxorepromicin (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. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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