G. R. Brown, A. Foubister, S. Freeman
Mar 4, 1997
Citations
0
Influential Citations
12
Citations
Quality indicators
Journal
Bioorganic & Medicinal Chemistry Letters
Abstract
Abstract Optimised quinuclidine squalene synthase (SQS) inhibitors are reported; 3-[2-(2-allyl-4-(2-ethoxy carbonylethyl)phenyl)ethynyl]quinuclidin-3-ol 1c, is a potent inhibitor of rat (KI = 6 nM) and human (KI = 43 nM) microsomal SQS; the oral ED50 of 1c, for the inhibition of rat cholesterol biosynthesis was 1.3±0.45 mg/kg and for the R-enantiomer 1m, 0.8±0.2 mg/kg, with the corresponding R-carboxylic acid 6a, being 0.9±0.25 mg/kg.