Article
Discovery of imidazolidine-2,4-dione-linked HIV protease inhibitors with activity against lopinavir-resistant mutant HIV.
Bioorganic & medicinal chemistry - 1 Oct 2006
Flosi William J, DeGoey David A, Grampovnik David J, Chen Hui-ju, Klein Larry L, Dekhtyar Tatyana, Masse Sherie, Marsh Kennan C, Mo Hong Mei, Kempf Dale
Abstract excerpt
A new series of HIV protease inhibitors has been designed and synthesized based on the combination of the (R)-(hydroxyethylamino)sulfonamide isostere and the cyclic urea component of lopinavir. The series was optimized by replacing the 6-membered cyclic urea linker with an imidazolidine-2,4-dione which readily underwent N-alkylation to incorporate various methylene-linked heterocycle groups that bind favorably in...
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