NOVEL C2-SYMMETRICAL PHENYLBORONIC ACID PINACOL ESTERS WITH A FEW TYPES OF LINKERS AND THEIR BIOLOGICAL ACTIVITIES
NOVEL C2-SYMMETRICAL PHENYLBORONIC ACID PINACOL ESTERS WITH A FEW TYPES OF LINKERS AND THEIR BIOLOGICAL ACTIVITIES
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DOI：
10.3987/com-17-13745
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发表时间：
2017-09-01
期刊：
影响因子：
0.6
通讯作者：
Sumoto, Kunihiro
中科院分区：
文献类型：
--
作者：
Furutachi, Makoto;Gondo, Toshiaki;Sumoto, Kunihiro
本文报道了新的C-2-对称环苯硼酸衍生物的合成及其生物活性。新的目标C-2-对称分子（1）获得良好至优异的产率通过原始酰胺键形成反应，使用报道的方法开始与氨基取代的苯基硼酸频哪醇酯2。为了评价抗菌和抗病毒活性，还制备了一些C-2-对称苯基硼酸酯类似物，如5和7，它们在接头连接处具有两个脲基团。构效关系研究的结果也被描述。
We report the preparation of new C-2-symmetrical cyclic phenylboronic acid derivatives and their biological activities. New targeted C-2-symmetrical molecules (1) were obtained in good to excellent yields by a primitive amide bond formation reaction using the reported method starting with amino-substituted phenylboronic acid pinacol esters 2. A few C-2-symmetrical phenylboronic acid ester analogues such as 5 and 7 that have two urea groups in the linker junction were also prepared in order to evaluate antibacterial and antiviral activities. The results of a structure-activity relationship study are also described.