Novel hydroxyphenylurea dual inhibitor against acyl-CoA: cholesterol acyltransferase (ACAT) and low density lipoprotein (LDL) oxidation as antiatherosclerotic agent.

Nakao K; Kubota H; Yasuhara M; Saito K; Suzuki T; Ohmizu H; Shimizu R

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Novel hydroxyphenylurea dual inhibitor against acyl-CoA: cholesterol acyltransferase (ACAT) and low density lipoprotein (LDL) oxidation as antiatherosclerotic agent.

机译：新型的针对酰基辅酶A的羟苯基脲双重抑制剂：胆固醇酰基转移酶（ACAT）和低密度脂蛋白（LDL）氧化作为抗动脉粥样硬化剂。

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Novel hydroxyphenylurea derivatives were synthesized and their inhibitory potency evaluated against acyl-CoA: cholesterol acyltransferase (ACAT). Quantitative structure activity relationship analysis revealed that their ACAT inhibitory activities were controlled by the hydrophobicity of the whole molecule. the substitution pattern of urea moiety, and the existence of carboxylic acid. The derivatives with strong activities inhibited foam cell formations. Moreover, these compounds showed antioxidative effects against low density lipoprotein (LDL), owing to their characteristic 3-lert-butyl-2-hydroxy-5-methoxyphenyl substructure. Based on the mechanism of atherosclerosis generation, this hydroxyphenylurea-type dual inhibitor against both ACAT and LDL oxidation is expected to be a promising drug for atherosclerosis.

机译：合成了新的羟苯基脲衍生物，并评估了其对酰基辅酶A：胆固醇酰基转移酶（ACAT）的抑制能力。定量结构活性关系分析表明，它们的ACAT抑制活性受整个分子的疏水性控制。脲部分的取代方式，以及羧酸的存在。具有强活性的衍生物抑制了泡沫孔的形成。此外，这些化合物由于其特征性的3-叔丁基-2-羟基-5-甲氧基苯基亚结构而对低密度脂蛋白（LDL）表现出抗氧化作用。基于动脉粥样硬化的产生机理，这种针对ACAT和LDL氧化的羟苯基脲类双重抑制剂有望成为一种有前途的动脉粥样硬化药物。

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来源
《Bioorganic and medicinal chemistry》 |2001年第4期|共9页
作者
Nakao K; Kubota H; Yasuhara M; Saito K; Suzuki T; Ohmizu H; Shimizu R;
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正文语种 eng
中图分类药学;生物化学;
关键词
Anisoles; Arteriosclerosis; Enzyme Inhibitors; Lipoproteins; LDL; Phenylurea Compounds; 茴香醚类; 动脉硬化; 酶抑制剂; 脂蛋白类; LDL; 苯脲化合物;

机译：Anisoles;Arteriosclerosis;Enzyme Inhibitors;Lipoproteins;LDL;Phenylurea Compounds;茴香醚类;动脉硬化;酶抑制剂;脂蛋白类;LDL;苯脲化合物;

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专利

1. Novel hydroxyphenylurea dual inhibitor against acyl-CoA: cholesterol acyltransferase (ACAT) and low density lipoprotein (LDL) oxidation as antiatherosclerotic agent. [J] . Nakao K, Kubota H, Yasuhara M, Bioorganic and medicinal chemistry . 2001,第4期

机译：新型的针对酰基辅酶A的羟苯基脲双重抑制剂：胆固醇酰基转移酶（ACAT）和低密度脂蛋白（LDL）氧化作为抗动脉粥样硬化剂。
2. Direct effect of an acyl-CoA: cholesterol acyltransferase inhibitor, F-1394, on atherosclerosis in apolipoprotein E and low density Lipoprotein receptor double knockout mice [J] . Tsuyoshi Chiwata, Katsumi Aragane, Koji Fujinami British Journal of Pharmacology . 2001,第7期

机译：酰基辅酶A的直接作用：胆固醇酰基转移酶抑制剂F-1394对载脂蛋白E和低密度脂蛋白受体双敲除小鼠的动脉粥样硬化
3. Novel 1,4-diarylpiperidine-4-methylureas as anti-hyperlipidemic agents: dual effectors on acyl-CoA:cholesterol O-acyltransferase and low-density lipoprotein receptor expression. [J] . Asano S, Ban H, Kino K, Bioorganic and Medicinal Chemistry Letters . 2009,第4期

机译：新型1,4-二芳基哌啶-4-甲基脲作为抗高氧化性药剂：酰基-CoA上的双重效应器：胆固醇O-酰基转移酶和低密度脂蛋白受体表达。
4. Changes of Vascular Wall and Total Cholesterol, High Density Lipoprotein, Oxidized low Density Lipoprotein, Nitric Monoxide and Lipide Peroxidation in Serum after Arcuate Nucleus Lesioned [C] . HE Ying-Ying, rnWANG Xiao-Chang, rnFAN Xiao-Yuan, The 1st International Symposium on Sectional and Imaging Anatomy . 2007

机译：弓形核病变后血清中血管壁和总胆固醇，高密度脂蛋白，氧化型低密度脂蛋白，一氧化氮和脂质过氧化的变化
5. Sortilin as a novel regulator of plasma cholesterol, very-low density lipoprotein secretion and LDL catabolism. [D] . Strong, Alanna. 2012

机译：Sortilin是一种新型的血浆胆固醇，极低密度脂蛋白分泌和LDL分解代谢调节剂。
6. Direct effect of an acyl-CoA:cholesterol acyltransferase inhibitor F-1394 on atherosclerosis in apolipoprotein E and low density lipoprotein receptor double knockout mice [O] . Tsuyoshi Chiwata, Katsumi Aragane, Koji Fujinami, 2001

机译：酰基辅酶A：胆固醇酰基转移酶抑制剂F-1394对载脂蛋白E和低密度脂蛋白受体双敲除小鼠的动脉粥样硬化的直接作用
7. Effects of F-1394, an Acyl-CoA:Cholesterol Acyltransferase (ACAT) Inhibitor, on ACAT Activity in HepG2 Cells and on Hepatic Secretion of Lipids in Triton WR-1339-Induced Hyperlipidemic Rats: Possible Role of Hepatic ACAT in Very Low Density Lipoprotein Secretion [O] . Katsumi Aragane, Jun Kusunoki, Tetsuya Kitamine, 1998

机译：F-1394，丙基 - CoA：胆固醇酰酰转移酶（ACAT）抑制剂，对HepG2细胞的ACAT活性以及Triton WR-1339诱导的高脂质虫大鼠肝脏分泌的影响：肝脏AcAT在非常低密度脂蛋白中的可能作用分泌

Novel hydroxyphenylurea dual inhibitor against acyl-CoA: cholesterol acyltransferase (ACAT) and low density lipoprotein (LDL) oxidation as antiatherosclerotic agent.

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