Sulfonamide derivatives of benzylamine block cholesterol biosynthesis in HepG2 cells: a new type of potent squalene epoxidase inhibitors.
Sulfonamide derivatives of ene-yne benzylamine 1 have been prepared and identified as a new class of potent SE inhibitors having demonstrated activity in HepG2 cells as cholesterol biosynthesis inhibitors.
Gotteland
J P
JP
Medicinal Chemistry Division, Centre de Recherche Pierre Fabre, Castres, France. cm4.crpf@pierre-fabre.imaginet.fr
Loubat
C
C
Planty
B
B
Junquéro
D
D
Delhon
A
A
Halazy
S
S
D000818:Animals; D000924:Anticholesteremic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001596:Benzylamines / Q000138:chemical synthesis* / Q000494:pharmacology; D002460:Cell Line; D002784:Cholesterol / Q000096:biosynthesis*; D004285:Dogs; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D008099:Liver / Q000201:enzymology; D010105:Oxygenases / Q000037:antagonists & inhibitors*; D051381:Rats; D050603:Squalene Monooxygenase; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology; D013552:Swine
D000924:Anticholesteremic Agents; D001596:Benzylamines; D004791:Enzyme Inhibitors; D013449:Sulfonamides; D002784:Cholesterol; D010105:Oxygenases; D050603:Squalene Monooxygenase