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本文引用的文献

1
Investigation of anti-dermatophytic effects of non-steroidal anti-inflammatory drugs on trichophyton mentagrophytes and epidermophyton floccosum.非甾体抗炎药对须癣毛癣菌和絮状表皮癣菌的抗皮肤癣菌作用研究。
Iran J Pharm Res. 2011 Summer;10(3):547-52.
2
Anti-inflammatory effects of fibrates: an overview.贝特类药物的抗炎作用：综述
Curr Med Chem. 2009;16(6):676-84. doi: 10.2174/092986709787458416.
3
Sila-haloperidol, a silicon analogue of the dopamine (D2) receptor antagonist haloperidol: synthesis, pharmacological properties, and metabolic fate.西拉氟哌啶醇，多巴胺（D2）受体拮抗剂氟哌啶醇的硅类似物：合成、药理性质及代谢命运。
ChemMedChem. 2008 Jan;3(1):152-64. doi: 10.1002/cmdc.200700205.
4
Peroxisome proliferator-activated receptors as transcriptional nodal points and therapeutic targets.过氧化物酶体增殖物激活受体作为转录节点和治疗靶点。
Circulation. 2007 Jan 30;115(4):518-33. doi: 10.1161/CIRCULATIONAHA.104.475673.
5
The role of the peroxisome proliferator-activated receptor-alpha (PPAR-alpha) in the regulation of acute inflammation.过氧化物酶体增殖物激活受体α（PPAR-α）在急性炎症调节中的作用。
J Leukoc Biol. 2006 May;79(5):999-1010. doi: 10.1189/jlb.0605341. Epub 2006 Feb 24.
6
Beneficial vascular and metabolic effects of peroxisome proliferator-activated receptor-alpha activators.过氧化物酶体增殖物激活受体α激活剂的有益血管和代谢作用。
Hypertension. 2005 Nov;46(5):1086-92. doi: 10.1161/01.HYP.0000187900.36455.4c. Epub 2005 Oct 17.
7
Silicon chemistry as a novel source of chemical diversity in drug design.硅化学作为药物设计中化学多样性的新来源。
Curr Opin Drug Discov Devel. 2003 Jul;6(4):526-43.
8
Roles of PPARs in health and disease.过氧化物酶体增殖物激活受体（PPARs）在健康与疾病中的作用。
Nature. 2000 May 25;405(6785):421-4. doi: 10.1038/35013000.
9
The PPARs: from orphan receptors to drug discovery.过氧化物酶体增殖物激活受体：从孤儿受体到药物发现
J Med Chem. 2000 Feb 24;43(4):527-50. doi: 10.1021/jm990554g.
10
Fatty acids, eicosanoids, and hypolipidemic agents identified as ligands of peroxisome proliferator-activated receptors by coactivator-dependent receptor ligand assay.通过共激活因子依赖性受体配体测定法鉴定为过氧化物酶体增殖物激活受体配体的脂肪酸、类二十烷酸和降血脂药物。
Mol Endocrinol. 1997 Jun;11(6):779-91. doi: 10.1210/mend.11.6.0007.

一种新型氯贝丁酯硅化类似物（西立贝特）的合成及其抗炎活性比较。

Synthesis of a Novel Siliconized Analog of Clofibrate (Silafibrate) and Comparison of their Anti-inflammatory Activities.

作者信息

Ziaee Mojtaba, Samini Morteza, Bolourtchian Mohammad, Ghaffarzadeh Mohammad, Ahmadi Maryam, Egbal Mohammad Ali, Khorrami Arash, Andalib Sina, Maleki-Dizaji Nasrin, Garjani Alireza

机构信息

Department of Pharmacology, Science & Research Branch, Islamic Azad University, Tehran, Iran.

Chemistry and Chemical Engineering Research Center of Iran, Tehran, Iran.

出版信息

Iran J Pharm Res. 2012 Winter;11(1):91-5.

PMID:25317189
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3876562/
Abstract

Fibrates, as hypolipidemic drugs known as agonists of peroxisome proliferator-activated receptors, diminish inflammatory responses. Studies have shown that incorporation of a silicon atom into a drug structure improves its pharmacological potency, modifies its selectivity toward a given target, or changes its metabolic rate, in addition to increasing the lipophilicity of the compounds. A siliconized analog of clofibrate, ethyl-2-methyl-2-(4-(trimethylsilyl)phenoxy)propionate was synthesized, whereby the chlorine atom in the phenoxy ring was replaced by a trimethylsilyl group. The anti-inflammatory effects of the siliconized analog (silafibrate) were evaluated in an air-pouch model of inflammation and compared with those of clofibrate. Oral administration of both drugs produced a significant anti-inflammatory action by reducing carrageenan induced pouch leukocyte recruitment, exudates production, and granulated tissue weight. The silicon isostere of clofibrate has improved anti-inflammatory properties.

摘要

贝特类药物作为过氧化物酶体增殖物激活受体激动剂类的降血脂药物，可减轻炎症反应。研究表明，将硅原子引入药物结构除了能增加化合物的亲脂性外，还能提高其药理活性、改变其对特定靶点的选择性或改变其代谢速率。合成了氯贝丁酯的硅化类似物，即2-甲基-2-(4-(三甲基硅基)苯氧基)丙酸乙酯，其中苯氧基环中的氯原子被三甲基硅基取代。在气囊炎症模型中评估了该硅化类似物（西立贝特）的抗炎作用，并与氯贝丁酯进行了比较。口服这两种药物均通过减少角叉菜胶诱导的气囊白细胞募集、渗出物产生和肉芽组织重量而产生显著的抗炎作用。氯贝丁酯的硅类似物具有更好的抗炎特性。