流感病毒唾液酸酶潜在抑制剂——过渡态类似物的合成
Synthesis of transition-state analogues as potential inhibitors of sialidase from Influenza virus.
作者信息
Driguez P A, Barrere B, Quash G, Doutheau A
机构信息
Laboratoire de Chimie Organique, Institut National des Sciences Appliquées, Villeurbanne, France.
出版信息
Carbohydr Res. 1994 Sep 15;262(2):297-310. doi: 10.1016/0008-6215(94)84186-1.
Sodium 5-acetamido-2,6-anhydro-3,4,5-trideoxy-D-manno-non-2-enonate (2) has been synthesized from N-acetyl-4-deoxy-neuraminic acid methyl ester (4). Sodium 2,6-anhydro-3-deoxy-L-arabino-hept-2-enonate (3), 4-acetamido-2,6-anhydro-3,4-dideoxy-L-arabino-hept-2-enonic acid (18e), and 4-acetamido-2,6-anhydro-3,4-dideoxy-L-ribo-hept-2-enonic acid (18a) have been prepared from L-arabinose. The above compounds were investigated as inhibitors of sialidase from Influenza virus. Only compound 2 showed a significant inhibitory activity (Ki 8 x 10(-2) mM) against the enzyme.
5-乙酰氨基-2,6-脱水-3,4,5-三脱氧-D-甘露糖-2-烯糖酸钠（2）由N-乙酰基-4-脱氧神经氨酸甲酯（4）合成。2,6-脱水-3-脱氧-L-阿拉伯糖-2-烯糖酸钠（3）、4-乙酰氨基-2,6-脱水-3,4-二脱氧-L-阿拉伯糖-2-烯糖酸（18e）和4-乙酰氨基-2,6-脱水-3,4-二脱氧-L-核糖-2-烯糖酸（18a）由L-阿拉伯糖制备。上述化合物作为流感病毒唾液酸酶抑制剂进行了研究。只有化合物2对该酶表现出显著的抑制活性（Ki 8×10⁻² mM）。
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