崇城大学DDS研究所紀要第1巻2017年
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derivatives having alkoxy and/or alkylamino groups and results of biological evaluation of their anti-herpes simplex virus type 1 (anti-HSV-1) activity and cytotoxic activity against Vero cells. New targeted symmetrical molecules were obtained by using a method starting with 2,4,6-trichloro-1,3,5-triazine (1). Among the synthesized compounds, CS-symmetrical tri-aliphatic alkylamino-substituted compound 6s showed high anti-HSV-1 activity (EC50 = 5.4 μM) and low cytotoxicity (CC50 > 200 μM). The results of an SAR study suggested that the presence of two hydrogen bond donor protons of sec-amine functionality in the molecule is an important structural factor for expression of potential anti-HSV-1 activities. Novel C2-Symmetrical Phenylboronic Acid Pinacol Esters with a Few Types of Linkers and Their Biological Activities Makoto Furutachi Toshiaki Gondo Saho Goto Saho Fuchigami Kenta Ako Yuki Oowada Kazumi Yokomizo Jian-Rong Zhou Tomohiro Ishizaki Takahiro Koga Nobuhiro Kashige Fumio Miake Kunihiro Sumoto Heterocycles. Vol.94(9), pp.1748-1758. 201729 We report the preparation of new C2-symmetrical cyclic phenylboronic acid derivatives and their biological activities. New targeted C2-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 C2-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

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