Author/Authors :
Anna Ax، نويسنده , , Advait A. Joshi، نويسنده , , Kristina M. Orrling، نويسنده , , Lotta Vrang، نويسنده , , Bertil Samuelsson، نويسنده , , Anders Hallberg، نويسنده , , Anders Karlén، نويسنده , , Mats Larhed، نويسنده ,
Abstract :
A set of 11 non-symmetric cyclic sulfamide HIV-1 protease inhibitors were synthesized and evaluated. The use of a key microwave-assisted silver(I) oxide mediated selective mono N-benzylation reaction enabled fast and straightforward synthesis. The Ki values of the new inhibitors ranged between 0.28 μM and >20 μM.
Keywords :
Benzylation , HIV-1 , Protease inhibitor , Palladium catalysis , Microwave
