Recently, a class of compounds bearing a β-diketo acid moiety have emerged as the most promising lead in anti-HIV-1 IN
drug discovery. It is believed that the β-diketo acid pharmacophoric motif could be
involved in a functional sequestration of one or both divalent metal ions, which are critical
cofactors at the enzyme catalytic site. This would subsequently block the transition state
of the IN-DNA complex. In this scenario, it is of paramount importance to acquire
information about the mode of action of diketo acids, which could then be useful in the design of new compounds as IN inhibitors
