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Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. CI-1011: an acyl sulfamate with unique cholesterol-lowering activity in animals fed noncholesterol-supplemented diets.

作者信息

Lee H T, Sliskovic D R, Picard J A, Roth B D, Wierenga W, Hicks J L, Bousley R F, Hamelehle K L, Homan R, Speyer C, Stanfield R L, Krause B R

机构信息

Department of Medicinal Chemistry, Radiochemistry, Parke-Davis Pharmaceutical Research, Division of Warner-Lambert Company, Ann Arbor, Michigan 48105, USA.

出版信息

J Med Chem. 1996 Dec 20;39(26):5031-4. doi: 10.1021/jm960674d.

DOI:10.1021/jm960674d
PMID:8978833
Abstract
摘要

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1
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. CI-1011: an acyl sulfamate with unique cholesterol-lowering activity in animals fed noncholesterol-supplemented diets.
J Med Chem. 1996 Dec 20;39(26):5031-4. doi: 10.1021/jm960674d.
2
Inhibitors of acyl-CoA:cholesterol O-acyltransferase. synthesis and pharmacological activity of (+/-)-2-dodecyl-alpha-phenyl-N-(2,4,6-trimethoxyphenyl)-2H-tetrazole-5- acetamide and structurally related tetrazole amide derivatives.酰基辅酶A:胆固醇O-酰基转移酶抑制剂。(±)-2-十二烷基-α-苯基-N-(2,4,6-三甲氧基苯基)-2H-四唑-5-乙酰胺及结构相关的四唑酰胺衍生物的合成与药理活性
J Med Chem. 1996 Jun 7;39(12):2354-66. doi: 10.1021/jm960170f.
3
Pharmacology of the ACAT inhibitor avasimibe (CI-1011).酰基辅酶A胆固醇酰基转移酶(ACAT)抑制剂阿伐西丁(CI-1011)的药理学
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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.杂环酰胺:酰基辅酶A:胆固醇O-酰基转移酶抑制剂,在多个物种中具有降胆固醇活性,在兔中具有抗动脉粥样硬化活性。
J Med Chem. 1996 Sep 27;39(20):3908-19. doi: 10.1021/jm9604033.
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Pharmacological profile of SMP-797, a novel acyl-coenzyme a: cholesterol acyltransferase inhibitor with inducible effect on the expression of low-density lipoprotein receptor.新型酰基辅酶A:胆固醇酰基转移酶抑制剂SMP-797的药理学特性及其对低密度脂蛋白受体表达的诱导作用
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Relationships between lipophilicity and biological activities in a series of indoline-based anti-oxidative acyl-CoA:cholesterol acyltransferase (ACAT) inhibitors.一系列基于吲哚啉的抗氧化酰基辅酶A:胆固醇酰基转移酶(ACAT)抑制剂的亲脂性与生物活性之间的关系。
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Acyl-coenzyme A:cholesterol acyltransferase inhibitor, avasimibe, stimulates bile acid synthesis and cholesterol 7alpha-hydroxylase in cultured rat hepatocytes and in vivo in the rat.酰基辅酶A:胆固醇酰基转移酶抑制剂阿伐西丁,在培养的大鼠肝细胞和大鼠体内均能刺激胆汁酸合成及胆固醇7α-羟化酶。
Hepatology. 1999 Aug;30(2):491-500. doi: 10.1002/hep.510300230.
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Inhibitors of acyl-CoA:cholesterol O-acyltransferase (ACAT) as hypocholesterolemic agents: synthesis and structure-activity relationships of novel series of sulfonamides, acylphosphonamides and acylphosphoramidates.
Bioorg Med Chem Lett. 1998 Feb 3;8(3):289-94. doi: 10.1016/s0960-894x(98)00011-0.
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Divergent pharmacologic activities of PD 132301-2 and CL 277,082, urea inhibitors of acyl-CoA:cholesterol acyltransferase.酰基辅酶A:胆固醇酰基转移酶的尿素抑制剂PD 132301-2和CL 277,082的不同药理活性。
J Pharmacol Exp Ther. 1993 Nov;267(2):734-43.
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Heterocyclic ureas: inhibitors of acyl-CoA:cholesterol O-acyltransferase as hypocholesterolemic agents.杂环脲类:酰基辅酶A:胆固醇O-酰基转移酶抑制剂作为降胆固醇药物。
J Med Chem. 1996 Oct 25;39(22):4382-95. doi: 10.1021/jm960404v.

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