CCR5, a member of G protein-coupled receptors superfamily, plays an important role in the HIV-1 entry process.
Antagonism of this receptor finally leads to the inhibition of R5 strains of HIV entry into the human cells. The identification
of CCR5 antagonists as antiviral agents will provide more option for HAART. Now, more than a decade after the
first small molecule CCR5 inhibitor was discovered, great achievements have been made. In this article, we will give a
brief introduction of several series of small molecule CCR5 antagonists, focused on their appealing structure evolution,
essential SAR information and thereof the enlightenment of strategies on CCR5 inhibitors design.