Synthesis of riccardin D derivatives as potent antimicrobial agents.
Synthesis of riccardin D derivatives as potent antimicrobial agents.
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DOI：
10.1016/j.bmcl.2016.06.006
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发表时间：
2016-08
影响因子：
2.7
通讯作者：
Bin Sun;Ming Zhang;Y. Li;Qing-wen Hu;Hong-Bo Zheng;Wenqiang Chang;H. Lou
中科院分区：
文献类型：
--
作者：
Bin Sun;Ming Zhang;Y. Li;Qing-wen Hu;Hong-Bo Zheng;Wenqiang Chang;H. Lou
介绍了一类新型抗菌分子--蓖麻素D衍生物的合成及生物活性评价。通过在Riccardin D的芳环上引入羟基、甲氧基和溴，实现了这些衍生物的结构多样化。这些化合物的抗菌性能被作为对临床分离的细菌和真菌的体外试验进行评估。在蓖麻素D的芳香族化合物中引入溴原子，得到了几种对甲氧西林敏感和耐药的金黄色葡萄球菌的MIC值在0.5~4μg/m L之间的强效抗菌化合物。抗真菌试验发现，化合物34对白色念珠菌的MIC值为2μg/mL，是最有效的分子。这一初步的生物学评价表明，这些新分子作为潜在的抗菌剂值得进一步研究。
We describe the synthesis and biological evaluation of riccardin D derivatives, a novel class of antimicrobial molecules. Structural diversification of these derivatives was achieved by introducing hydroxy, methoxy, and bromine into the aromatic rings of riccardin D. The antimicrobial evaluation of these compounds was performed as in vitro assays against clinically isolated bacteria and fungi. The introduction of bromine atom into the areneBof riccardin D led to several strongly active antibacterial compounds with a MIC value ranging from 0.5 to 4 μg/mL for Staphylococcus aureus, both methicillin-sensitive and -resistant strains. Antifungal tests found compound34was the most potent molecule with a MIC value of 2 μg/mL against Candida albicans. This initial biological evaluation suggests that these novel molecules merit further investigation as potential antimicrobial agents.