title: Inhibitors of acyl-CoA:cholesterol O-acyltransferase (ACAT) as hypocholesterolemic agents: synthesis and structure-activity relationships of novel series of sulfonamides, acylphosphonamides and acylphosphoramidates.
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.
authors.affiliation: Department of Medicinal Chemistry, Parke-Davis Pharmaceutical Research, Division of Warner-Lambert Company, Ann Arbor, Michigan 48105, USA.
authors.forename: H T
authors.initials: HT
authors.lastname: Lee
authors.forename: W H
authors.initials: WH
authors.lastname: Roark
authors.forename: J A
authors.initials: JA
authors.lastname: Picard
authors.forename: D R
authors.initials: DR
authors.lastname: Sliskovic
authors.forename: B D
authors.initials: BD
authors.lastname: Roth
authors.forename: R L
authors.initials: RL
authors.lastname: Stanfield
authors.forename: K L
authors.initials: KL
authors.lastname: Hamelehle
authors.forename: R F
authors.initials: RF
authors.lastname: Bousley
authors.forename: B R
authors.initials: BR
authors.lastname: Krause
mesh_terms: D000818:Animals; D000924:Anticholesteremic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008861:Microsomes / Q000187:drug effects / Q000201:enzymology; D009943:Organophosphorus Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011817:Rabbits; D002785:Sterol O-Acyltransferase / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000924:Anticholesteremic Agents; D004791:Enzyme Inhibitors; D009943:Organophosphorus Compounds; D013449:Sulfonamides; D002785:Sterol O-Acyltransferase