Sun Chun-Lai, Pang Rui-Fang, Zhang Hang, Yang Ming
National Research Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100083, People's Republic of China.
Bioorg Med Chem Lett. 2005 Jul 1;15(13):3257-62. doi: 10.1016/j.bmcl.2005.04.057.
Twenty-four 4-hydroxypyrone derivatives were synthesized with a facile synthetic method to develop novel HIV protease inhibitors. Most of them were shown to display good antiviral activities in SIV-infected CEM cells. The introduction of alpha-naphthylmethyl group to C-6 of 5,6-dihydropyran-2-ones led to an effective antiviral compound that showed an EC(50) value at 1.7 microM with a therapeutic index of 46.
采用简便的合成方法合成了24种4-羟基吡喃衍生物，以开发新型HIV蛋白酶抑制剂。其中大多数在感染SIV的CEM细胞中显示出良好的抗病毒活性。在5,6-二氢吡喃-2-酮的C-6位引入α-萘甲基基团得到了一种有效的抗病毒化合物，其EC(50)值为1.7 microM，治疗指数为46。
