Novel Lopinavir Analogues Incorporating Heterocyclic Replacements of Six-Member Cyclic Urea. Synthesis and Structure—Activity Relationships

The HIV protease inhibitor ABT-378 (lopinavir) has a six-member cyclic urea in the P-2 position. A series of analogues in which the six-member cyclic urea is replaced by various heterocycles was synthesized and the structure-activity relationships explored.