title: Synthesis and biological evaluation of symmetrical 2,4,6-trisubstituted 1,3,5-triazine derivatives.
abstract: We describe the synthesis and biological evaluation of newly designed 2,4,6-trisubstituted symmetrical 1,3,5-triazine (TAZ) derivatives. Among the tested trisubstituted symmetrical TAZ derivatives, various C3- or CS-symmetrical alkoxy-amino-substituted TAZ derivatives showed significant antiviral activity against herpes simplex virus type 1 (HSV-1) and/or cytotoxic activity against Vero cells. The structure-activity relationships for anti-HSV-1 activity of these symmetrical 2,4,6-trisubstituted TAZ derivatives are also described. Experimental results indicated that a CS-symmetrical TAZ structure with introduction of two alkoxy groups and one amine moiety seems to be the minimally required structure for anti-HSV-1 activity.
authors.affiliation: Faculty of Pharmaceutical Sciences, Fukuoka University, 8–19–1 Nanakuma, Jonan-ku, Fukuoka 814–0180, Japan.
authors.forename: Nobuko
authors.initials: N
authors.lastname: Mibu
authors.forename: Kazumi
authors.initials: K
authors.lastname: Yokomizo
authors.forename: Satoshi
authors.initials: S
authors.lastname: Takemura
authors.forename: Nami
authors.initials: N
authors.lastname: Ueki
authors.forename: Saki
authors.initials: S
authors.lastname: Itohara
authors.forename: Jianrong
authors.initials: J
authors.lastname: Zhou
authors.forename: Takeshi
authors.initials: T
authors.lastname: Miyata
authors.forename: Kunihiro
authors.initials: K
authors.lastname: Sumoto
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002522:Chlorocebus aethiops; D006561:Herpes Simplex / Q000188:drug therapy; D018259:Herpesvirus 1, Human / Q000187:drug effects*; D006801:Humans; D013329:Structure-Activity Relationship; D014227:Triazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D014709:Vero Cells
chemical_list: D000998:Antiviral Agents; D014227:Triazines