Gerrish David, Kim In Chul, Kumar Dange V, Austin Harry, Garrus Jennifer E, Baichwal Vijay, Saunders Michael, McKinnon Rena S, Anderson Mark B, Carlson Robert, Arranz-Plaza Esther, Yager Kraig M
Myriad Pharmaceuticals Inc., 320 Wakara Way, Salt Lake City, UT 84108, USA.
Bioorg Med Chem Lett. 2008 Dec 15;18(24):6377-80. doi: 10.1016/j.bmcl.2008.10.098. Epub 2008 Oct 25.
Efforts towards developing orally bioavailable HIV-1 maturation inhibitors starting from betulinic acid 1 are described. SAR resulted in improved potency, physicochemical properties, and enhanced oral absorption in rats.
描述了从桦木酸1开始开发口服生物可利用的HIV-1成熟抑制剂的努力。构效关系研究带来了更高的效力、更好的物理化学性质以及大鼠口服吸收的增强。