Sulfonamide derivatives of benzylamine block cholesterol biosynthesis in HepG2 cells: a new type of potent squalene epoxidase inhibitors

J P Gotteland; C Loubat; B Planty; D Junquéro; A Delhon; S Halazy

doi:10.1016/s0960-894x(98)00213-3

Sulfonamide derivatives of benzylamine block cholesterol biosynthesis in HepG2 cells: a new type of potent squalene epoxidase inhibitors

Bioorg Med Chem Lett. 1998 Jun 2;8(11):1337-42. doi: 10.1016/s0960-894x(98)00213-3.

Authors

J P Gotteland¹, C Loubat, B Planty, D Junquéro, A Delhon, S Halazy

Affiliation

¹ Medicinal Chemistry Division, Centre de Recherche Pierre Fabre, Castres, France. cm4.crpf@pierre-fabre.imaginet.fr

PMID: 9871762
DOI: 10.1016/s0960-894x(98)00213-3

Abstract

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.

MeSH terms

Animals
Anticholesteremic Agents / chemical synthesis*
Anticholesteremic Agents / pharmacology
Benzylamines / chemical synthesis*
Benzylamines / pharmacology
Cell Line
Cholesterol / biosynthesis*
Dogs
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / pharmacology
Humans
Liver / enzymology
Oxygenases / antagonists & inhibitors*
Rats
Squalene Monooxygenase
Sulfonamides / chemical synthesis*
Sulfonamides / pharmacology
Swine

Substances

Anticholesteremic Agents
Benzylamines
Enzyme Inhibitors
Sulfonamides
Cholesterol
Oxygenases
Squalene Monooxygenase