"Structure-Based Design of HIV Protease Inhibitors: 5,6-dihydro-4-hydroxy-2-pyrones As Effective, Nonpeptidic Inhibitors."

According to the authors' abstract of an article published in Journal of Medicinal Chemistry, "From a broad screening program, the 4-hydroxycoumarin phenprocoumon (I) was previously identified as a lead template with HIV protease inhibitory activity. The crystal structure of phenprocoumon/HIV protease complex initiated a structure-based design effort that initially identified the 4-hydroxy-2-pyrone U-96988 (II) as a first-generation clinical candidate for the potential treatment of HIV infection. Based upon the crystal structure of the 4-hydroxy-2-pyrone III/HIV protease complex, a series of analogues incorporating a 5,6-dihydro-4-hydroxy-2-pyrone template were studied. It was...

Want to see the full article?

• Purchase this article for only $3.00