Author/Authors :
Ishaiahu Shechter، نويسنده , , Peide Gu، نويسنده , , Guojian Jiang، نويسنده , , Thomas J. Onofrey، نويسنده , , Reginald O. Cann، نويسنده , , Alfredo Castro، نويسنده , , Thomas A. Spencer، نويسنده ,
Abstract :
Zwitterions such as farnesyl sulfobetaine 8 are a new type of inhibitor of squalene synthase that, while maintaining overall neutrality, mimic both the carbocationic and anionic moieties of presumed reaction intermediates. The most effective zwitterionic sulfobetaines discovered to date are aromatic derivatives 17 (IC50 = 2 μM) and 20 (IC50 = 5 μM).