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Synthesis and Antiviral Activities of Some 2,4,6-Trisubstituted 1,3,5-Triazines

2014; Pharmaceutical Society of Japan; Volume: 62; Issue: 10 Linguagem: Inglês

10.1248/cpb.c14-00421

1347-5223

Nobuko Mibu, Kazumi Yokomizo, Airi Koga, Miyuki Honda, Kou Mizokami, Hiroyuki Fujii, Norimasa Ota, Ai Yuzuriha, Kanji Ishimaru, Jian-Rong Zhou, Takeshi Miyata, Kunihiro Sumoto,

Click Chemistry and Applications

We describe the synthesis and results of biological evaluation of newly designed 2,4,6-trisubstituted symmetrical 1,3,5-triazine (TAZ) derivatives. Among the tested trisubstituted TAZ derivatives, some CS-symmetrical alkoxy-amino-substituted TAZ derivatives, including 7ggp and 6dpp, showed significant antiviral activity against herpes simplex virus type 1 (HSV-1). The compound with the highest level of antiviral activity was C3-symmetrical trialkoxy-TAZ derivative 4bbb, which showed a considerably high selectivity index (IC50/EC50=256.6). The structure-activity relationships for anti-HSV-1 activity of the tested 2,4,6-trisubstituted TAZ derivatives are also described.