Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2016-05-04 , DOI: 10.1016/j.bmcl.2016.05.003 Xing Zhang 1 , Omar Khalidi 2 , So Young Kim 3 , Ruitong Wang 1 , Victor Schultz 1 , Brady F Cress 2 , Richard A Gross 4 , Mattheos A G Koffas 5 , Robert J Linhardt 6
A series of 5,7-dihydroxyflavanone derivatives were efficiently synthesized. Their antimicrobial efficacy on Gram-negative, Gram-positive bacteria and yeast were evaluated. Among these compounds, most of the halogenated derivatives exhibited the best antimicrobial activity against Gram-positive bacteria, the yeast Saccharomyces cerevisiae, and the Gram-negative bacterium Vibrio cholerae. The cytotoxicities of these compounds were low as evaluated on HepG2 cells using a cell viability assay. This study suggests that halogenated flavanones might represent promising pharmacological candidates for further drug development.
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抗菌剂5,7-二羟基黄烷酮衍生物的合成及生物学评价
高效合成了一系列5,7-二羟基黄烷酮衍生物。评估了它们对革兰氏阴性菌、革兰氏阳性菌和酵母菌的抗菌功效。在这些化合物中,大多数卤化衍生物对革兰氏阳性菌、酿酒酵母和革兰氏阴性菌霍乱弧菌表现出最好的抗菌活性。使用细胞活力测定对 HepG2 细胞进行评估时,这些化合物的细胞毒性较低。这项研究表明,卤代黄烷酮可能代表了进一步药物开发的有希望的药理学候选者。