Syntheses and biological evaluations of carbosilane dendrimers uniformly functionalized with sialyl alpha(2-->3) lactose moieties as inhibitors for human influenza viruses.
A series of carbosilane dendrimers uniformly functionalized with sialyl lactose moieties (Neu5Ac alpha2-->3Gal beta1-->4Glc) was systematically synthesized, and biological evaluations for anti-influenza virus activity using the glycodendrimers were performed. The results suggested that the glycodendrimers had unique biological activities depending on the form of their core frame, and Dumbbell(1)6-amide type glycodendrimer 7 showed particularly strong inhibitory activities against human influenza viruses [A/PR/8/34 (H1N1) and A/Aichi/2/68 (H3N2)]. The results suggested that the structure-activity relationship (SAR) on the glycolibrary against various influenza viruses was observed, and dumbbell-shaped dendrimers as supporting carbohydrate moieties were found to be the most suitable core scaffolds in this study.
Oka
Hiroyuki
H
Division of Material Science, Graduate School of Science and Engineering, Saitama University, Sakura, Saitama 338-8570, Japan.
Onaga
Tomotsune
T
Koyama
Tetsuo
T
Guo
Chao-Tan
CT
Suzuki
Yasuo
Y
Esumi
Yasuaki
Y
Hatano
Ken
K
Terunuma
Daiyo
D
Matsuoka
Koji
K
D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002460:Cell Line; D050091:Dendrimers / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D004285:Dogs; D004912:Erythrocytes / Q000166:cytology / Q000821:virology; D006384:Hemagglutination / Q000187:drug effects; D006461:Hemolysis / Q000187:drug effects; D006801:Humans; D053118:Influenza A Virus, H1N1 Subtype / Q000187:drug effects / Q000472:pathogenicity; D053122:Influenza A Virus, H3N2 Subtype / Q000187:drug effects / Q000472:pathogenicity; D009980:Influenza A virus / Q000187:drug effects* / Q000472:pathogenicity; D007251:Influenza, Human / Q000188:drug therapy; D007668:Kidney / Q000166:cytology / Q000821:virology; D007785:Lactose / Q000737:chemistry; D015394:Molecular Structure; D019158:N-Acetylneuraminic Acid / Q000737:chemistry; D012821:Silanes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000998:Antiviral Agents; D050091:Dendrimers; D012821:Silanes; C504072:carbosilane; D019158:N-Acetylneuraminic Acid; D007785:Lactose