HETEROCYCLES

■ Hybrid Linker Mode C2-Symmetrical 1,3,5-Triazine Derivatives and Their Biological Evaluation

Shunsuke Shimomura, Kazumi Yokomizo, Jian-Rong Zhou, Kaori Ota, Nobuko Mibu, Makoto Furutachi, and Kunihiro Sumoto*

*Faculty of Pharmaceutical Sciences, Fukuoka University, 8-19-1 Nanakuma, Jonan-ku, Fukuoka 814-0180, Japan

Abstract

We report the preparation of some new multivalent hybrid-type C2-symmetrical molecules having a methylene linker group and 1,3,5-triazine (TAZ) moieties in the molecule and the results of biological evaluation of their anti-herpes simplex virus type 1 (anti-HSV-1) activity and cytotoxic activity against Vero cells. Some of the mid-sized C2-symmetrical multivalent hybrid-type molecules (3a) showed considerably high levels of anti-HSV-1 activity (EC50 = 28.8 ~ 32.0 μM) with low levels of cytotoxicity (CC50 = > 200 μM) against Vero cells. Among the tested hybrid-type TAZ derivatives, we reconfirmed that the hybrid-type C2-symmetrical multivalent molecule (3a-4) is an interesting candidate in the search for new hybrid-type multivalent mid-sized antiviral compounds.