2', 6'-Dimethylphenoxyacetyl: A New Achiral High Affinity P3-P2 Ligand for Peptidomimetic-Based HIV Protease Inhibitors

…, V Gorys, C Grand-Maître, D Lamarre…

文献索引：Beaulieu, Pierre L.; Anderson, Paul C.; Cameron, Dale R.; Croteau, Gilbert; Gorys, Vida; Grand-Maitre, Chantal; Lamarre, Daniel; Liard, Francine; Paris, William; Plamondon, Louis; Soucy, Francois; Thibeault, Diane; Wernic, Dominik; Yoakim, Christiane; Pav, Susan; Tong, Liang Journal of Medicinal Chemistry, 2000 , vol. 43, # 6 p. 1094 - 1108

全文：HTML全文

被引用次数: 35

摘要

Starting from palinavir (1), our lead HIV protease inhibitor, we have discovered a new series of truncated analogues in which the P3-P2 quinaldic-valine portion of 1 was replaced by 2', 6'-dimethylphenoxyacetyl. With EC50's in the 1-2 nM range, some of these compounds are among the most potent inhibitors of HIV replication in vitro, reported to date. One of the most promising members in this series (compound 27, BILA 2185 BS) exhibited a favorable ...