- Comparative study of new and known thienyl derivatives of ene-yne benzylamine as mammalian squalene epoxidase inhibitors
-
Analogs of the well-known squalene epoxidase inhibitor (SE) NB-598 (2) have been prepared and tested as cholesterol biosynthesis inhibitors in HepG2 cells. Among the compounds tested, the vinylthiophene analog 4 and the tertiary amide derivative of thiophene 8 emerged as potent human SE inhibitors and probably bind to the enzyme in a very similar manner as NB-598 (2). Surprisingly enough, compounds 4 and 8, contrary to NB-598, are poor inhibitors of rat SE, thus further demonstrating major differences between mammalian enzymes from different species.
- Gotteland,Junquero,Oms,Delhon,Halazy
-
p. 333 - 342
(2007/10/03)
-