Synthesis of (+)-biotin derivatives as HIV-1 protease inhibitors

Article abstract of DOI:10.1016/0960-894X(96)00233-8

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 K(i) of 0.50 μM and antiviral IC₉₀ of 7 μM. The (+