Preparation and Antiviral Activity of Some New C3- and CS-Symmetrical Tri-Substituted Triazine Derivatives Having Benzylamine Substituents

We report the preparation of new C3- and CS-symmetrical molecules constructed on a triazine (TAZ) template. Anti-herpes simplex virus type 1 (anti-HSV-1) and cytotoxic activities against Vero cells of synthesized TAZ derivatives were evaluated. The results suggested that the presence of an electron-...

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Veröffentlicht in:Chemical & pharmaceutical bulletin 2018/08/01, Vol.66(8), pp.830-838
Hauptverfasser: Mibu, Nobuko, Yokomizo, Kazumi, Sano, Marina, Kawaguchi, Yuuna, Morimoto, Kenta, Shimomura, Syunsuke, Sato, Ryo, Hiraga, Nozomi, Matsunaga, Aya, Zhou, Jian-Rong, Ohata, Tomonori, Aki, Hatsumi, Sumoto, Kunihiro
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Sprache:eng
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Zusammenfassung:We report the preparation of new C3- and CS-symmetrical molecules constructed on a triazine (TAZ) template. Anti-herpes simplex virus type 1 (anti-HSV-1) and cytotoxic activities against Vero cells of synthesized TAZ derivatives were evaluated. The results suggested that the presence of an electron-donating group(s) on the benzene ring in benzylamine groups on the TAZ template is an important structural factor for expressing a high level of anti-HSV-1 activity and low cytotoxicity for these C3 types of TAZ derivatives. Among the tested TAZ derivatives, compounds 4f and 7h showed the highest anti HSV-1 activities (EC50=0.98 and 1.23 µM, respectively) and low cytotoxic activities to Vero cells (50% cytotoxic concentration (CC50)=292.2 and >200 µM, respectively).
ISSN:0009-2363
1347-5223
DOI:10.1248/cpb.c18-00274