166957-84-2Relevant academic research and scientific papers
Heterocyclic derivatives
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, (2008/06/13)
Compounds of formula (I) wherein R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 are joined together so that CR1 14 CR2 is a double bond; X is selected from --Ch2 CH
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.
