Discovery of a small molecule inhibitor through interference with the gp120–CD4 interaction

A series of piperazine derivatives were designed and synthesised as gp120–CD4 inhibitors. SAR studies led to the discovery of potent inhibitors in a cell based anti viral assay represented by compounds 9 and 28. The rat pharmacokinetic and antiviral profiles of selected compounds are also presented.

Graphical abstractIdentification and SAR of a series of piperazine derivatives as inhibitors of the gp120–CD4 interaction is described.Figure optionsDownload full-size imageDownload as PowerPoint slide