title: Cyclopentanedi- and tricarboxylic acids as squalene synthase inhibitors: syntheses and evaluation.
abstract: Based on earlier lead squalene synthase inhibitor A-87049 (3) and zaragozic acids, a series of cyclopentanedi- and tricarboxylic acids were synthesized and evaluated against the enzyme. Some exhibited good potency and SAR revealed the importance of conformation and substitution pattern of these synthetic inhibitors.
authors.affiliation: Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, IL 60064, USA.
authors.forename: W
authors.initials: W
authors.lastname: Shen
authors.forename: D S
authors.initials: DS
authors.lastname: Garvey
authors.forename: J
authors.initials: J
authors.lastname: Cohen
authors.forename: H
authors.initials: H
authors.lastname: Stein
authors.forename: S H
authors.initials: SH
authors.lastname: Rosenberg
mesh_terms: D000818:Animals; D003517:Cyclopentanes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D003998:Dicarboxylic Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013186:Farnesyl-Diphosphate Farnesyltransferase / Q000037:antagonists & inhibitors*; D007202:Indicators and Reagents; D007536:Isomerism; D008862:Microsomes, Liver / Q000201:enzymology; D008958:Models, Molecular; D008968:Molecular Conformation; D015394:Molecular Structure; D051381:Rats; D013329:Structure-Activity Relationship; D014233:Tricarboxylic Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D003517:Cyclopentanes; D003998:Dicarboxylic Acids; D004791:Enzyme Inhibitors; D007202:Indicators and Reagents; D014233:Tricarboxylic Acids; D013186:Farnesyl-Diphosphate Farnesyltransferase