期刊
CHEMICAL & PHARMACEUTICAL BULLETIN
卷 64, 期 12, 页码 1769-1780出版社
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/cpb.c16-00682
关键词
tris(2-aminoethyl)amine; C-3 symmetry; C-s symmetry; anti-herpes simplex virus type 1; tripodal receptor-type; plaque reduction assay
We report the preparation of new tripodal receptor-type C-3- and C-s-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 mu M) and low cytotoxicity (50% cytotoxic concentration (CC50)=>200 mu M). 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.
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