Progress on diketo acid HIV-1 integrase inhibitors

HIV-1 integrase catalyzes the integration of proviral DNA into the genome of the host cell,an essential step for viral replication,thus inhibition of integrase catalytic activity represents a rational strategy for the treatment of HIV-1 infection.At present,a lot of HIV-1 integrase inhibitors have been designed and synthesized,and some of them are studied currently in clinical trials.In a view of chemical structure,most of the HIV-1 integrase inhibitors reported belong to the class of diketo acids or their bioisosters.Recent advances on diketo acid HIV-1 integrase inhibitors are reviewed in this paper.