Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells

Integrase is essential for human immunodeficiency virus-type 1 (HIV-1) repl ication; however, potent inhibition of the isolated enzyme in biochemical a ssays has not readily translated into antiviral activity in a manner consis tent with inhibition of integration. In this report, we describe diketo aci d inhibitors of HIV-1 integrase that manifest antiviral activity as a conse quence of their effect on integration. The antiviral activity of these comp ounds is due exclusively to inhibition of one of the two catalytic function s of integrase, strand transfer.