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二氢-[1H]-喹啉-2-酮作为视黄酸X受体（RXR）激动剂用于潜在治疗血脂异常

Dihydro-[1H]-quinolin-2-ones as retinoid X receptor (RXR) agonists for potential treatment of dyslipidemia.

作者信息

Lagu Bharat, Lebedev Rimma, Pio Barbara, Yang Maria, Pelton Patricia D

机构信息

Johnson and Johnson Pharmaceutical Research and Development, Cranbury, NJ 08512, USA.

出版信息

Bioorg Med Chem Lett. 2007 Jun 15;17(12):3491-6. doi: 10.1016/j.bmcl.2007.01.049. Epub 2007 Jan 25.

DOI:10.1016/j.bmcl.2007.01.049
PMID:17490875
Abstract

A number of RXR modulators with novel structural features were synthesized and screened in the functional assays. The synthesis and the structure-activity relationship within the series of compounds will be presented. Some in vivo data generated in the models for dyslipidemia and diabetes will also be presented.

摘要

合成了多种具有新颖结构特征的RXR调节剂，并在功能测定中进行了筛选。将介绍该系列化合物的合成及构效关系。还将展示在血脂异常和糖尿病模型中产生的一些体内数据。

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Dihydro-[1H]-quinolin-2-ones as retinoid X receptor (RXR) agonists for potential treatment of dyslipidemia.二氢-[1H]-喹啉-2-酮作为视黄酸X受体（RXR）激动剂用于潜在治疗血脂异常
Bioorg Med Chem Lett. 2007 Jun 15;17(12):3491-6. doi: 10.1016/j.bmcl.2007.01.049. Epub 2007 Jan 25.
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Selective androgen receptor modulators based on a series of 7H-[1,4]oxazino[3,2-g]quinolin-7-ones with improved in vivo activity.基于一系列具有改善的体内活性的7H-[1,4]恶嗪并[3,2-g]喹啉-7-酮的选择性雄激素受体调节剂。
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RXR partial agonist produced by side chain repositioning of alkoxy RXR full agonist retains antitype 2 diabetes activity without the adverse effects.通过烷氧基RXR全激动剂的侧链重排产生的RXR部分激动剂保留了抗2型糖尿病活性且无不良反应。
J Med Chem. 2015 Jan 22;58(2):912-26. doi: 10.1021/jm501863r. Epub 2014 Dec 17.

引用本文的文献

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A Novel Biphenyl-based Chemotype of Retinoid X Receptor Ligands Enables Subtype and Heterodimer Preferences.一种新型的基于联苯的视黄酸X受体配体化学类型可实现亚型和异二聚体偏好。
ACS Med Chem Lett. 2019 Aug 16;10(9):1346-1352. doi: 10.1021/acsmedchemlett.9b00306. eCollection 2019 Sep 12.
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α-Lithiation and electrophilic substitution of 1,4,4-trimethyl-3,4-dihydroquinolin-2-one.1,4,4-三甲基-3,4-二氢喹啉-2(1H)-酮的α-锂化和亲电取代反应。
Molecules. 2010 Oct 29;15(11):7742-9. doi: 10.3390/molecules15117742.