Kim C U, Chen X, Mendel D B
Gilead Sciences, Foster City, CA 94404, USA.
Antivir Chem Chemother. 1999 Jul;10(4):141-54. doi: 10.1177/095632029901000401.
Influenza virus neuraminidase (NA) catalyses the cleavage of sialic acid residues terminally linked to glycoproteins and glycolipids and plays an important role in the replication of the virus. Recently, several potent NA inhibitors have been synthesized based on the rational design of mimicking the transition state of the sialic acid cleavage. Zanamivir and oseltamivir (GS 4104, the prodrug of GS 4071) have emerged as promising influenza NA inhibitors for the treatment and prophylaxis of human influenza virus infection. This review describes the recent work toward the discovery and development of influenza NA inhibitors.
流感病毒神经氨酸酶(NA)催化末端连接至糖蛋白和糖脂的唾液酸残基的裂解,并在病毒复制中起重要作用。最近,基于模拟唾液酸裂解过渡态的合理设计,合成了几种有效的NA抑制剂。扎那米韦和奥司他韦(GS 4104,GS 4071的前体药物)已成为用于治疗和预防人类流感病毒感染的有前景的流感NA抑制剂。本文综述了流感NA抑制剂发现与开发的近期研究进展。