Synthesis and biological evaluation of novel allophenylnorstatine-based HIV-1 protease inhibitors incorporating high affinity P2-ligands
作者:Arun K. Ghosh、Sandra Gemma、Elena Simoni、Abigail Baldridge、D. Eric Walters、Kazuhiko Ide、Yasushi Tojo、Yasuhiro Koh、Masayuki Amano、Hiroaki Mitsuya
DOI:10.1016/j.bmcl.2009.11.123
日期:2010.2
A series of stereochemically defined cyclic ethers as P2-ligands were incorporated in an allophenylnorstatine-based isostere to provide a new series of HIV-1proteaseinhibitors. Inhibitors 3b and 3c, containing conformationally constrained cyclic ethers, displayed impressive enzymatic and antiviral properties and represent promising lead compounds for further optimization.