Kim Ronald M, Rouse Elizabeth A, Chapman Kevin T, Schleif William A, Olsen David B, Stahlhut Mark, Rutkowski Carrie A, Emini Emilio A, Tata James R
Department of Basic Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.
Bioorg Med Chem Lett. 2004 Sep 20;14(18):4651-4. doi: 10.1016/j.bmcl.2004.06.092.
HIV-1 protease inhibitors (PI's) bearing 1,3,4-oxadiazoles at the P1' position were prepared by a novel method involving the diastereoselective installation of a carboxylic acid and conversion to the P1' heterocycle. The compounds are picomolar inhibitors of native HIV-1 protease, with most of the compounds maintaining excellent antiviral activity against a panel of PI-resistant strains.
通过一种新方法制备了在P1'位置带有1,3,4-恶二唑的HIV-1蛋白酶抑制剂（PI），该方法涉及非对映选择性引入羧酸并转化为P1'杂环。这些化合物是天然HIV-1蛋白酶的皮摩尔级抑制剂，大多数化合物对一组耐PI的毒株保持优异的抗病毒活性。
