Design and optimisation of potent gp120-CD4 inhibitors

The synthesis and structure–activity relationship of a series of novel gp120-CD4 inhibitors are described. Pharmacokinetic studies and antiviral spectrum assessment of lead compounds led to the identification of compound 36, a potent gp120-CD4 inhibitor which exhibited antiviral potency across a spectrum of 25 clade B isolates.

Graphical abstractThe synthesis and SAR of a series of novel gp120-CD4 inhibitors are described. Pharmacokinetic studies and antiviral spectrum assessment of lead compounds led to the identification of compound 36.Figure optionsDownload full-size imageDownload as PowerPoint slide