Synthesis and influenza virus inhibitory activities of carbosilane dendrimers peripherally functionalized with hemagglutinin-binding Peptide.

作者: Ken Hatano , Teruhiko Matsubara , Yosuke Muramatsu , Masakazu Ezure , Tetsuo Koyama

DOI: 10.1021/JM5007676

关键词:

摘要: A series of carbosilane dendrimers uniformly functionalized with hemagglutinin (HA) binding peptide (sialic acid-mimic peptide, Ala-Arg-Leu-Pro-Arg) was systematically synthesized, and their anti-influenza virus activity evaluated. The carbosilane-based dendrimers, unlike sialylated cannot be digested by neuraminidases. exhibited intriguing biological activities depending on the form core frame, a dumbbell-type dendrimer showing particularly strong inhibitory against two human influenza viruses, A/PR/8/34 (H1N1) A/Aichi/2/68 (H3N2). IC50 values for both strains were 0.60 μM, highest among HA-binding derivatives. results suggest that dumbbell-shaped is most suitable scaffold dendrimers.

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