A new class of diketo acids constructed on pyridinone scaffolds, designed as inhibitors of HTV replication through inhibition of HIV
integrase, is described. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS and ARC, either as the compounds, or as pharmaceutically acceptable salts, with pharmaceutically acceptable carriers, used alone or in combination with antivirals, immunomodulators,
antibiotics, vaccines, and other therapeutic agents, especially other anti- HIV compounds (including other anti-HIV
integrase agents), which can be used to create combination anti-HIV cocktails. Methods of treating AIDS and ARC and methods of treating or preventing infection by HIV are also described. Compounds of the present application include those of formula I and include tautomers, regioisomers, geometric isomers, and pharmaceutically acceptable salts thereof, wherein the pyridinone
scaffold and R groups are as otherwise defined in the specification. These are combined, with any number of typical other anti-HIV agents (including other
integrase-based anti-HIV agents) and other combination therapeutic agents described herein, to provide an
effective treatment modality for HIV infections, including AIDS and ARC.