3-Hydroxy-4-oxo-4H-pyrido[1,2-a]pyrimidine-2-carboxylates--a new class of HIV-1 integrase inhibitors.

A new class of inhibitors of HIV-1 integrase has been optimized to provide selective and highly efficient strand transfer inhibition.

Tetrazole thioacetanilides: potent non-nucleoside inhibitors of WT HIV reverse transcriptase and its K103N mutant.

A series of aryltetrazolylacetanilides was synthesized and evaluated as HIV-1 non-nucleoside reverse transcriptase inhibitors on wild-type virus and on the clinically relevant K103N mutant strain. Extensive SAR investigation led to potent compounds, with nanomolar activity on K103N, and orally bioavailable in rats.