Inhibitors of acyl-CoA:cholesterol O-acyltransferase (ACAT) as hypocholesterolemic agents: synthesis and structure-activity relationships of novel series of sulfonamides, acylphosphonamides and acylphosphoramidates

H T Lee; W H Roark; J A Picard; D R Sliskovic; B D Roth; R L Stanfield; K L Hamelehle; R F Bousley; B R Krause

doi:10.1016/s0960-894x(98)00011-0

Inhibitors of acyl-CoA:cholesterol O-acyltransferase (ACAT) as hypocholesterolemic agents: synthesis and structure-activity relationships of novel series of sulfonamides, acylphosphonamides and acylphosphoramidates

Bioorg Med Chem Lett. 1998 Feb 3;8(3):289-94. doi: 10.1016/s0960-894x(98)00011-0.

Authors

H T Lee¹, W H Roark, J A Picard, D R Sliskovic, B D Roth, R L Stanfield, K L Hamelehle, R F Bousley, B R Krause

Affiliation

¹ Department of Medicinal Chemistry, Parke-Davis Pharmaceutical Research, Division of Warner-Lambert Company, Ann Arbor, Michigan 48105, USA.

PMID: 9871672
DOI: 10.1016/s0960-894x(98)00011-0

Abstract

Sulfoacetic acid, phosphoramidate, and phosphoramide analogs of the ACAT inhibitors, CI-999 and CI-1011 were synthesized. The structure-activity relationships of these compounds as ACAT inhibitors are described.

MeSH terms

Animals
Anticholesteremic Agents / chemical synthesis*
Anticholesteremic Agents / chemistry
Anticholesteremic Agents / pharmacology
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology
Microsomes / drug effects
Microsomes / enzymology
Organophosphorus Compounds / chemical synthesis*
Organophosphorus Compounds / chemistry
Organophosphorus Compounds / pharmacology
Rabbits
Sterol O-Acyltransferase / antagonists & inhibitors*
Structure-Activity Relationship
Sulfonamides / chemical synthesis*
Sulfonamides / chemistry
Sulfonamides / pharmacology

Substances

Anticholesteremic Agents
Enzyme Inhibitors
Organophosphorus Compounds
Sulfonamides
Sterol O-Acyltransferase