Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai 201203, China.
Carbohydr Res. 2011 Oct 18;346(14):2126-35. doi: 10.1016/j.carres.2011.07.028. Epub 2011 Aug 9.
A series of novel oligorhamnoside derivatives (1-10) and naturally occurring cleistrioside-5 were synthesized and evaluated for their in vitro antibacterial activities. Among them, dirhamnoside derivative 7 and cleistrioside-5 displayed similar antibacterial profiles and exhibited moderate to good inhibitory activities on bacterial growth against a panel of Gram-positive bacteria (MICs ≤ 4-32 μg/mL). The results revealed that these two compounds showed selectivity towards bacterial species strictly, without being affected by the antibiotic-resistant/susceptible properties of one species, which suggested that they might have the potential to avoid antibiotic cross-resistance. In addition, the preliminary SARs of this type of oligorhamnoside derivatives on the antibacterial activities were determined.
合成了一系列新型寡鼠李糖苷衍生物(1-10)和天然存在的Cleistrioside-5,并评估了它们的体外抗菌活性。其中,二鼠李糖苷衍生物 7 和 Cleistrioside-5 表现出相似的抗菌谱,对一系列革兰氏阳性菌的生长具有中等至良好的抑制活性(MICs≤4-32μg/mL)。结果表明,这两种化合物对细菌具有严格的选择性,不受一种细菌的抗生素耐药/敏感特性的影响,这表明它们可能具有避免抗生素交叉耐药的潜力。此外,还确定了这类寡鼠李糖苷衍生物对抗菌活性的初步构效关系。