166959-22-4Relevant academic research and scientific papers
Novel optimised quinuclidine squalene synthase inhibitors
Brown, George R.,Foubister, Alan J.,Freeman, Susan,McTaggart, Fergus,Mirrlees, Donald J.,Reid, Alan C.,Smith, Graham J.,Taylor, Melvyn J.,Thomason, Douglas A.,Whittamore, Paul R. O.
, p. 597 - 600 (2007/10/03)
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.
