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Synthesis and anti-Influenza evaluation of polyvalent sialidase inhibitors bearing 4-guanidino-Neu5Ac2en derivatives

2002; Elsevier BV; Volume: 12; Issue: 15 Linguagem: Inglês

10.1016/s0960-894x(02)00330-x

1464-3405

Takeshi Honda, Shuku Yoshida, Masami Arai, Takeshi Masuda, Makoto Yamashita,

Diabetes and associated disorders

We synthesized polyvalent sialidase inhibitors bearing 4-guanidino-Neu5Ac2en analogues on the polyglutamic acid back bone, via a spacer of alkyl ether at the C-7 position. These multivalent conjugates 9 and 10 showed enhancement of antiviral activity against infuenza A virus and more potent efficacy in vivo relative to a monomeric sialidase inhibitor.