Bioorganic and Medicinal Chemistry Letters p. 597 - 600 (1997)
Update date:2022-09-26
Topics:
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.
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.
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