2. Academic Validation
  3. Repromicin derivatives with potent antibacterial activity against Pasteurella multocida

Repromicin derivatives with potent antibacterial activity against Pasteurella multocida

  • J Med Chem. 1997 Mar 14;40(6):1041-5. doi: 10.1021/jm960435q.
J W McFarland 1,  S J Hecker,  B H Jaynes,  M R Jefson,  K M Lundy,  C B Vu,  E A Glazer,  S A Froshauer,  S F Hayashi,  B J Kamicker,  C P Reese,  J A Olson
Affiliations

Affiliation

  • 1 Central Research Division, Pfizer Inc., Groton, Connecticut 06340, USA. mcfarland@pfizer.com
PMID: 9083494 DOI: 10.1021/jm960435q
Abstract

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.

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