Andrews D M, Cherry P C, Humber D C, Jones P S, Keeling S P, Martin P F, Shaw C D, Swanson S
Department of Medicinal Chemistry, Glaxo-Wellcome Medicines Research Centre, Gunnels Wood Road, Herts, SG1 2NY, Stevenage, UK.
Eur J Med Chem. 1999 Jul-Aug;34(7-8):563-74. doi: 10.1016/s0223-5234(00)80026-4.
Analogues of 4-Guanidino-Neu5Ac2en (Zanamivir) have been prepared containing carbamate substituents at the 7-hydroxy position. (4S,5R,6R)-5-Acetylamino-6-[1R-[(6-aminohexyl)carbamoyloxy]-2R,3-dihydroxypropyl]-4-guanidino-5,6-dihydro-4H-pyran-2carboxylic acid and (4S,5R,6R)-5-Acetylamino-6-[1R-[heptylcarbamoyloxy]-2R,3-dihydroxypropyl]-4-guanidino-5,6-dihydro4H-pyran2-carboxylic acid were the two analogues possessing activity comparable to Zanamivir, showing potent inhibition of influenza virus sialidases and good antiviral activity in vitro.
已制备出7-羟基位置含有氨基甲酸酯取代基的4-胍基-Neu5Ac2en（扎那米韦）类似物。（4S，5R，6R）-5-乙酰氨基-6-[1R-[(6-氨基己基)氨甲酰氧基]-2R，3-二羟基丙基]-4-胍基-5，6-二氢-4H-吡喃-2-羧酸和（4S，5R，6R）-5-乙酰氨基-6-[1R-[庚基氨甲酰氧基]-2R，3-二羟基丙基]-4-胍基-5，6-二氢-4H-吡喃-2-羧酸是两种活性与扎那米韦相当的类似物，在体外显示出对流感病毒唾液酸酶的强效抑制作用和良好的抗病毒活性。
