含4-胍基-唾液酸烯丙酯衍生物的多价唾液酸酶抑制剂的合成及抗流感活性评价
Synthesis and anti-influenza evaluation of polyvalent sialidase inhibitors bearing 4-guanidino-Neu5Ac2en derivatives.
作者信息
Honda Takeshi, Yoshida Shuku, Arai Masami, Masuda Takeshi, Yamashita Makoto
机构信息
Medicinal Chemistry Research Laboratories, Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan.
出版信息
Bioorg Med Chem Lett. 2002 Aug 5;12(15):1929-32. doi: 10.1016/s0960-894x(02)00330-x.
Abstract
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.
摘要
我们通过在C-7位引入烷基醚间隔基，在聚谷氨酸主链上合成了带有4-胍基-Neu5Ac2en类似物的多价唾液酸酶抑制剂。相对于单体唾液酸酶抑制剂，这些多价缀合物9和10对甲型流感病毒显示出抗病毒活性增强以及在体内更有效的功效。
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