title: Antiviral Activity and Molecular Geometry of Some New Symmetrical Tris(aminoalkyl)amine Derivatives.
abstract: We report the preparation of new tripodal receptor-type C3- and CS-symmetrical molecules constructed on a tris(2-aminoethyl)amine (TAEA) template. Both the anti-herpes simplex virus type 1 (anti-HSV-1) activity and cytotoxic activity of synthesized receptor-type derivatives were evaluated in order to find a characteristic structural feature for these bioactivities of compounds. Among the compounds of synthesized symmetrical TAEA-related derivatives, compound 13k showed high anti-HSV-1 activity (50% effective concentration (EC50)=16.7 µM) and low cytotoxicity (50% cytotoxic concentration (CC50)=>200 µM). The presence of a hydrogen bond donor proton in the molecule is thought to be an important structural factor for expressing potential anti-HSV-1 activities.
authors.affiliation: Faculty of Pharmaceutical Sciences, Fukuoka University.
authors.forename: Nobuko
authors.initials: N
authors.lastname: Mibu
authors.forename: Kazumi
authors.initials: K
authors.lastname: Yokomizo
authors.forename: Kana
authors.initials: K
authors.lastname: Murakami
authors.forename: Yurika
authors.initials: Y
authors.lastname: Ono
authors.forename: Masato
authors.initials: M
authors.lastname: Ishimaru
authors.forename: Marie
authors.initials: M
authors.lastname: Otsubo
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Inao
authors.forename: Yutaro
authors.initials: Y
authors.lastname: Ono
authors.forename: Jian-Rong
authors.initials: JR
authors.lastname: Zhou
authors.forename: Kunihiro
authors.initials: K
authors.lastname: Sumoto
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects; D002522:Chlorocebus aethiops; D004305:Dose-Response Relationship, Drug; D005029:Ethylenediamines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D018259:Herpesvirus 1, Human / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D014709:Vero Cells
chemical_list: D000998:Antiviral Agents; D005029:Ethylenediamines; C099539:tris(2-aminoethyl)amine