Synthesis of pyrimidine and quinolone conjugates as a scaffold for dual inhibitors of HIV reverse transcriptase and integrase

A series of conjugates combining a pyrimidine and a quinolone moiety were designed and synthesized. The assay results show that these compounds demonstrate both anti-RT activity and anti-IN activity and therefore provide a useful scaffold for identifying inhibitors with balanced dual activities.

Graphical abstractA series of conjugates combining a pyrimidine and a quinolone moiety were designed and synthesized. These compounds are active against RT and IN and therefore provide a useful scaffold for identifying inhibitors with balanced dual activities.Figure optionsDownload full-size imageDownload as PowerPoint slide