新型基于全苯异亮氨酰基 HIV-1 蛋白酶抑制剂的合成与生物评价，其中包含高亲和力的 P2 配体。
Synthesis and biological evaluation of novel allophenylnorstatine-based HIV-1 protease inhibitors incorporating high affinity P2-ligands.
机构信息
Departments of Chemistry and Medicinal Chemistry, Purdue University, West Lafayette, IN 47907, United States.
出版信息
Bioorg Med Chem Lett. 2010 Feb 1;20(3):1241-6. doi: 10.1016/j.bmcl.2009.11.123. Epub 2009 Dec 5.
Abstract
A series of stereochemically defined cyclic ethers as P2-ligands were incorporated in an allophenylnorstatine-based isostere to provide a new series of HIV-1 protease inhibitors. Inhibitors 3b and 3c, containing conformationally constrained cyclic ethers, displayed impressive enzymatic and antiviral properties and represent promising lead compounds for further optimization.
摘要
一系列立体化学定义明确的环状醚作为 P2-配体被引入到基于别异亮氨酸的等排体中，以提供一系列新的 HIV-1 蛋白酶抑制剂。含有构象受限环状醚的抑制剂 3b 和 3c 表现出令人印象深刻的酶和抗病毒性质，是进一步优化的有前途的先导化合物。
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