Amide-containing diketoacids as HIV-1 integrase inhibitors: Synthesis, structure–activity relationship analysis, and biological activity

HIV-1 integrase, which catalyzes the integration of the viral genome into the cellular chromosome, is an essential enzyme for retroviral replication, and represents an attractive and validated target in the development of therapeutics against AIDS. In this paper, 17 amide-containing novel diketoacids were designed and synthesized, and their ability to inhibit HIV-1 integrase was tested. The structure–activity relationships were also analyzed.

A series of novel amide-containing diketoacids were designed and synthesized to develop potent HIV integrase inhibitors. Their inhibition of HIV integrase was tested and the structure–activity relationships were discussed.Figure optionsDownload as PowerPoint slide