Honda Takeshi, Masuda Takeshi, Yoshida Shuku, Arai Masami, Kobayashi Yoshiyuki, Yamashita Makoto
Medicinal Chemistry Research Laboratories, Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan.
Bioorg Med Chem Lett. 2002 Aug 5;12(15):1921-4. doi: 10.1016/s0960-894x(02)00328-1.
Substitution of 7-OH by small hydrophobic groups on zanamivir resulted in the retaining of low nanomolar inhibitory activities against not only influenza A virus sialidase but also influenza A virus in cell culture. These compounds were prepared by treatment of the corresponding 7-substituted sialic acids derived from 4-modified N-acetyl-D-mannosamine (ManNAc) using enzyme-catalyzed aldol condensation.
扎那米韦上的7-羟基被小的疏水基团取代后，不仅对甲型流感病毒唾液酸酶，而且对细胞培养中的甲型流感病毒都保留了低纳摩尔抑制活性。这些化合物是通过使用酶催化的羟醛缩合反应处理由4-修饰的N-乙酰-D-甘露糖胺（ManNAc）衍生的相应7-取代唾液酸来制备的。
