Synthesis of riccardin D derivatives as potent antimicrobial agents

Sun Bin; Zhang Ming; Li Ying; Hu Qing-wen; Zheng Hong-bo; Chang Wen-qiang; Lou Hong-xiang

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Synthesis of riccardin D derivatives as potent antimicrobial agents

机译：蓖麻毒素D衍生物的合成作为有效的抗菌剂

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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 arene B of riccardin D led to several strongly active antibacterial compounds with a MIC value ranging from 0.5 to 4 mu g/mL for Staphylococcus aureus, both methicillin-sensitive and -resistant strains. Antifungal tests found compound 34 was the most potent molecule with a MIC value of 2 mu g/mL against Candida albicans. This initial biological evaluation suggests that these novel molecules merit further investigation as potential antimicrobial agents. (C) 2016 Elsevier Ltd. All rights reserved.

机译：我们描述了riccardin D衍生物，一类新型的抗菌分子的合成和生物学评估。这些衍生物的结构多样化是通过将羟基，甲氧基和溴引入蓖麻毒素D的芳环中实现的。这些化合物的抗菌评估是针对临床分离的细菌和真菌的体外测定。将溴原子引入到蓖麻毒素D的芳烃B中，产生了几种强活性抗菌化合物，对金黄色葡萄球菌（对甲氧西林敏感和耐药的菌株）的MIC值为0.5至4μg / mL。抗真菌试验发现化合物34是最有效的分子，对白色念珠菌的MIC值为2μg / mL。最初的生物学评估表明，这些新型分子作为潜在的抗菌剂值得进一步研究。（C）2016 Elsevier Ltd.保留所有权利。

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《Bioorganic and Medicinal Chemistry Letters》 |2016年第15期|共4页
作者
Sun Bin; Zhang Ming; Li Ying; Hu Qing-wen; Zheng Hong-bo; Chang Wen-qiang; Lou Hong-xiang;
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正文语种 eng
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关键词
Bisbibenzyl; Derivatives; Antimicrobial; Anti-MRSA; Anti-fungal;

机译：双联苄;衍生物;抗菌;抗MRSA;抗真菌;

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1. Synthesis of riccardin D derivatives as potent antimicrobial agents [J] . Sun Bin, Zhang Ming, Li Ying, Bioorganic and Medicinal Chemistry Letters . 2016,第15期

机译：蓖麻毒素D衍生物的合成作为有效的抗菌剂
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Synthesis of riccardin D derivatives as potent antimicrobial agents

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