A series of novel pleuromutilin derivatives embracing 7H-pyrrolo[2,3-d]pyrimidine moiety were synthesized and evaluated for their in vitro antibacterial activity against Gram-positive and Gram-negative pathogens as well as in vivo efficacy in lethal systemic infected mice. Most compounds displayed good in vitro potency against MSSA, MRSA, MSSE, MRSE and E. faecium (MIC = 0.0625–4 μg/mL), especially 15a, 15b and 15o showed excellent activity that even more active than the comparator valnemulin. The in vivo efficacy investigation exhibited compound 15a (ED₅₀ = 16.0 mg/kg) had comparable activity to valnemulin (ED₅₀ = 13.5 mg/kg). The results provided by the dose-response study demonstrated 15a can supply infected mice with 70% survival rate at dose of 40 mg/kg via intragastric (i.g.) administration.

合成了一系列包含 7 H-吡咯并[2,3- d ]嘧啶部分的新型截短侧耳素衍生物，并评估了它们对革兰氏阳性和革兰氏阴性病原体的体外抗菌活性以及在致死性全身感染小鼠中的体内功效。大多数化合物在体外表现出良好的抗 MSSA、MRSA、MSSE、MRSE 和E的效力。屎肠球菌(MIC = 0.0625–4 μg/mL)，特别是15a 、 15b和15o显示出优异的活性，甚至比比较剂伐尼莫林更活跃。体内功效研究显示化合物15a (ED ₅₀ = 16.0 mg/kg)具有与伐尼莫林(ED ₅₀ = 13.5 mg/kg)相当的活性。剂量反应研究的结果表明， 15a通过灌胃 (ig) 剂量 40 mg/kg 可以为感染小鼠提供 70% 的存活率。