Evaluation of secondary amide replacements in a series of CCR5 antagonists as a means to increase intrinsic membrane permeability. Part 1: Optimization of gem-disubstituted azacycles

Replacement of a secondary amide with an N-acyl or N-sulfonyl gem-disubstituted azacyle in a series of CCR5 antagonists led to the identification of compounds with excellent in vitro HIV antiviral activity and increased intrinsic membrane permeability.

Graphical abstractReplacement of a secondary amide with an N-acyl or N-sulfonyl gem-disubstituted azacycle in a series of CCR5 antagonists led to the identification of compounds with excellent in vitro HIV antiviral activity and increased membrane permeability.Figure optionsDownload full-size imageDownload as PowerPoint slide