Spirodiketopiperazine-based CCR5 antagonists: Improvement of their pharmacokinetic profiles

Spirodiketopiperazine-based CCR5 antagonists, showing improved pharmacokinetic profiles without reduction in antagonist activity, were designed and synthesized. We also demonstrate the anti-HIV activity of a representative compound 12, as measured in a p24 assay.

Spirodiketopiperazine-based CCR5 antagonists, which showed improved pharmacokinetic (PK) profiles without reduction of the antagonist activity, were identified.Figure optionsDownload as PowerPoint slide