Author/Authors :
Qi Han، نويسنده , , Jennifer Lafontaine، نويسنده , , Lee T. Bacheler، نويسنده , , Marlene M. Rayner، نويسنده , , Ronald M. Klabe، نويسنده , , Susan Erickson-Viitanen، نويسنده , , Patrick Y. S. Lam، نويسنده ,
Abstract :
Several bis-N-alkylated (+)-biotin derivatives were synthesized and evaluated for activities against HIV-1 protease. The most potent inhibitor, 2D, synthesized in two steps from (+)-biotin, has Ki of 0.50 μM and antiviral IC90 of 7 μM. The (+)-biotin analogs in general have good translations from enzymatic Ki to antiviral cell assay IC90.
