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

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

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

Affiliation

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

Bioorg Med Chem Lett ; 8(3): 289-94, 1998 Feb 03.

Article in En | MEDLINE | ID: mdl-9871672

ABSTRACT

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.

Subject(s)

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

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Collection: 01-internacional Database: MEDLINE Main subject: Organophosphorus Compounds / Sulfonamides / Sterol O-Acyltransferase / Enzyme Inhibitors / Anticholesteremic Agents Limits: Animals Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 1998 Document type: Article Affiliation country: United States

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