Search Results - "Bousley, Richard"
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Substituted oxazolidinones as novel NPC1L1 ligands for the inhibition of cholesterol absorption
Published in Bioorganic & medicinal chemistry (15-01-2008)“…This manuscript describes the synthesis and evaluation of a series of oxazolidinone-based NPC1L1 ligands for the inhibition of cholesterol absorption…”
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Heterocyclic Ureas: Inhibitors of Acyl-CoA:Cholesterol O-Acyltransferase as Hypocholesterolemic Agents
Published in Journal of medicinal chemistry (25-10-1996)“…A series of diaryl-substituted heterocyclic ureas was prepared, and their ability to inhibit acyl-CoA:cholesterol O-acyltransferase (ACAT) in vitro and to…”
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Inhibitors of Acyl-CoA:Cholesterol O-Acyltransferase. 17. Structure−Activity Relationships of Several Series of Compounds Derived from N-Chlorosulfonyl Isocyanate
Published in Journal of medicinal chemistry (15-03-1996)“…Several series of acyl-CoA:cholesterol O-acyltransferase inhibitors were prepared by the stepwise addition of nitrogen, oxygen, and sulfur nucleophiles to…”
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CI-1011 lowers lipoprotein(a) and plasma cholesterol concentrations in chow-fed cynomolgus monkeys
Published in Atherosclerosis (1998)“…Lipoprotein(a) (Lp(a)), which is generated through the covalent association of apolipoprotein(a) (apo(a)) and apo B-100-LDL, is an independent risk factor for…”
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Inhibitors of Acyl-CoA:Cholesterol Acyltransferase (ACAT). 7. Development of a Series of Substituted N-Phenyl-N'-[(1-phenylcyclopentyl)methyl]ureas with Enhanced Hypocholesterolemic Activity
Published in Journal of medicinal chemistry (01-05-1994)“…We recently described our initial structure-activity relationship (SAR) studies on a series of N-phenyl-N'-aralkyl- and N-phenyl-N'-(1-phenylcycloalkyl)ureas…”
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α-Substituted Malonester Amides: Tools To Define the Relationship between ACAT Inhibition and Adrenal Toxicity
Published in Journal of medicinal chemistry (26-02-1998)“…We prepared a series of α-substituted malonester amides that were evaluated for their ability to inhibit acyl-CoA:cholesterol O-acyl transferase activity in…”
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Antithrombotic effect of LB-30057 (CI-1028), a new synthetic thrombin inhibitor, in a rabbit model of thrombosis: Comparison with inogatran
Published in Journal of thrombosis and thrombolysis (01-02-2001)“…LB-30057 (CI-1028) is a novel, orally bioavailable, direct thrombin inhibitor with a Ki of 0.38 nM against human thrombin. The effects of LB-30057 on thrombus…”
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Heterocyclic Amides: Inhibitors of Acyl-CoA:Cholesterol O-Acyl Transferase with Hypocholesterolemic Activity in Several Species and Antiatherosclerotic Activity in the Rabbit
Published in Journal of medicinal chemistry (27-09-1996)“…A series of heterocyclic amides were synthesized and evaluated as inhibitors of acyl-CoA:cholesterol O-acyltransferase (ACAT) in vitro and for cholesterol…”
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Tetrazole-substituted ureas as inhibitors of acyl-CoA:cholesterol O-acyltransferase (ACAT). A novel preparation of ureas from weakly nucleophilic amines
Published in Bioorganic & medicinal chemistry letters (06-08-1996)“…A novel series of tetrazole-substituted ureas 2 were prepared from weakly nucleophilic amines using a new coupling method. The ureas were found to potently…”
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Inhibitors of Acyl-CoA:Cholesterol O-Acyltransferase. 11. Structure-Activity Relationships of Several Series of Compounds Derived from N-(Chlorocarbonyl) Isocyanate
Published in Journal of medicinal chemistry (01-07-1994)“…Five series of compounds (4-9) derived from N-(chlorocarbonyl) isocyanate have been synthesized and evaluated for their ability to inhibit the enzyme…”
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Effect of the ACAT inhibitor CI-976 on plasma cholesterol concentrations and distribution in hamsters fed zero- and low-cholesterol diets
Published in Clinical biochemistry (01-10-1992)“…The overall objective of the present study was to determine if the ACAT inhibitor CI-976 can lower plasma cholesterol in hamsters fed zero or low, "human-like"…”
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Inhibitors of Acyl-CoA:Cholesterol O-Acyltransferase. Synthesis and Pharmacological Activity of (±)-2-Dodecyl-α-phenyl-N-(2,4,6-trimethoxyphenyl)-2H-tetrazole-5-acetamide and Structurally Related Tetrazole Amide Derivatives
Published in Journal of medicinal chemistry (07-06-1996)“…A series of tetrazole amide derivatives of (±)-2-dodecyl-α-phenyl-N-(2,4,6-trimethoxyphenyl)-2H-tetrazole-5-acetamide (1) was prepared and evaluated for their…”
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The antithrombotic effects of CI-1028, an orally bioavailable direct thrombin inhibitor, in a canine model of venous and arterial thrombosis
Published in Journal of thrombosis and thrombolysis (01-12-2000)“…Direct thrombin inhibitors represent a new class of drug that may offer a therapeutic alternative for the treatment and prevention of thrombembolic conditions,…”
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Effects of Intravenous Enoxaparin and Intravenous Inogatran in an Electrolytic Injury Model of Venous Thrombosis in the Dog
Published in Journal of thrombosis and thrombolysis (01-11-1998)“…The objective of this study was to compare the effectiveness of the low molecular weight heparin, enoxaparin (Lovenox((R))), and inogatran (a direct thrombin…”
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Effects of Quinapril, a New Angiotensin Converting Enzyme Inhibitor, on Left Ventricular Failure and Survival in the Cardiomyopathic Hamster: Hemodynamic, Morphological, and Biochemical Correlates
Published in Circulation research (01-05-1991)“…The effect of chronic therapy with quinapril on the temporal progression of left ventricular failure and survival was assessed in the CHF 146 cardiomyopathic…”
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Inhibitors of acyl-CoA: Cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 13. Design, synthesis and biological evaluation of tetrazole anilides as potent inhibitors of ACAT in vitro and hypocholesterolemic agents in vivo
Published in Bioorganic & medicinal chemistry letters (02-02-1995)“…The syntheses and biological activities for anilides derived from 2-phenyl-2-(dodecyl-2H-tetrazol-5-yl)acetic acid are described. Evidence is provided that one…”
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