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.

中文翻译：

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具有针对多杀巴斯德氏菌的强效抗菌活性的雷米霉素衍生物。

用多官能胺对瑞前霉素的还原胺化反应已产生了新的大环内酯类抗菌剂，其中一些在体外和小鼠感染模型中均对革兰氏阴性病原多杀性巴斯德氏菌具有很高的效力。该发现的关键要素是认识到，在某些已知的大环内酯类药物中，增加亲脂性会导致体内活性降低。选择一种repromicin衍生物20- [N- [3-（二甲基氨基）-丙基] -NL-丙氨酰氨基] -20-脱氧orepro micin（35）进行高级评估。以5 mg / kg的剂量皮下注射一次可控制猪诱发的巴氏杆菌病和牛诱发的呼吸道疾病。