College of Pharmacy, Hebei University of Chinese Medicine, Shijiazhuang 050200, China.
College of Chemical and Pharmaceutical Engineering, Hebei University of Science and Technology, Shijiazhuang 050018, China.
J Asian Nat Prod Res. 2021 Feb;23(2):123-137. doi: 10.1080/10286020.2020.1713764. Epub 2020 Feb 6.
We described the design, synthesis and antimicrobial activities of novel pleuromutilin derivatives with substituted piperazine substrate. Minimum inhibitory concentration (MIC) was used to evaluate the activity of the derivatives against six bacteria , and compound was potent against and with the MIC value of 0.0625 μg/ml. and showed similar activity to positive control drugs (tiamulin, erythromycin) against with the MIC value of 0.125 μg/ml. The binding mode of compound and tiamulin to the ribosome pocket showed the correlation between binding parameters and the antibacterial activity, and more bonds and stronger combination could effectively enhance the activity of compounds.[Formula: see text].
我们描述了具有取代哌嗪底物的新型截短侧耳素衍生物的设计、合成和抗菌活性。最小抑菌浓度（MIC）用于评估衍生物对六种细菌的活性，化合物对 和 具有很强的活性，MIC 值为 0.0625μg/ml。 和 对 与阳性对照药物（泰妙菌素、红霉素）的活性相似，MIC 值为 0.125μg/ml。化合物 和泰妙菌素与核糖体口袋的结合模式表明结合参数与抗菌活性之间存在相关性，更多的键和更强的结合可以有效增强化合物的活性。[化学式：见正文]。
