ANTIVIRAL ACTIVITIES OF SOME NEW 2,4,6-TRISUBSTITUTED 1,3,5-TRIAZINES HAVING ALKOXY AND/OR ALKYLAMINO GROUPS

作者：Mibu Nobuko; Yokomizo Kazumi; Yuzuriha Ai; Otsubo Marie; Kawaguchi Yuna; Sumo Marina; Sakai Izumi; Nakayama Keita; Zhou Jian Rong; Sumotol Kunihiro^*

来源：Heterocycles, 2017, 94(9): 1653-1677.

DOI：10.3987/COM-17-13735

We report the preparation of C-3- and C-S-symmetrical 2,4,6-trisubstituted 1,3,5-triazine 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, C-S-symmetrical tri-aliphatic alkylamino-substituted compound 6s showed high anti-HSV-1 activity (EC50 = 5.4 mu M) and low cytotoxicity (CC50 > 200 mu M). 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.

• 出版日期2017-9-1