Synthesis and Biological Evaluation of N-(5-(2,5-dimethyl-phenoxy)-2,2dimethylpentyl)-benzamide Derivatives as Novel Farnesoid X Receptor (FXR) Antagonist

Nian Siyun; Yu Zhenpeng; Tan Xiangduan; Gan Xia; Huang Mohan; Zhou Yihuan; Wang Guoping

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Synthesis and Biological Evaluation of N-(5-(2,5-dimethyl-phenoxy)-2,2dimethylpentyl)-benzamide Derivatives as Novel Farnesoid X Receptor (FXR) Antagonist

机译：N-（5-（2,5-二甲基 - 苯氧基）-2,2二甲基戊基） - 苄酰胺衍生物作为新型法呢X受体（FXR）拮抗剂的合成及生物学评价

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Background: Dyslipidemia is a serious threat to human health. The objective of our research was to develop effective FXR antagonists against dyslipidemia.

机译：背景：血脂血症是对人类健康的严重威胁。我们研究的目的是对血脂血症的有效的FXR拮抗剂进行效果。

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来源
《Letters in drug design & discovery》 |2018年第9期|共14页
作者
Nian Siyun; Yu Zhenpeng; Tan Xiangduan; Gan Xia; Huang Mohan; Zhou Yihuan; Wang Guoping;
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作者单位

China State Inst Pharmaceut Ind Shanghai Inst Pharmaceut Ind Shanghai 201203 Peoples R China;

YangZhou Aurisco Pharmaceut Co Ltd Yangzhou 225100 Jiangsu Peoples R China;

Guilin Med Univ Coll Pharm Guilin 541004 Peoples R China;

China State Inst Pharmaceut Ind Shanghai Inst Pharmaceut Ind Shanghai 201203 Peoples R China;

Guilin Med Univ Coll Pharm Guilin 541004 Peoples R China;

Guilin Med Univ Coll Pharm Guilin 541004 Peoples R China;

China State Inst Pharmaceut Ind Shanghai Inst Pharmaceut Ind Shanghai 201203 Peoples R China;

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原文格式 PDF
正文语种 eng
中图分类生药学（天然药物学）;
关键词
Hypolipidemic activity; FXR antagonists; synthesis; structure activity relationship; gugglesterone; molecular docking;

机译：低血脂活性;FXR拮抗剂;合成;结构活动关系;GUGGLENTONE;分子对接;

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1. Synthesis and Biological Evaluation of N-(5-(2,5-dimethyl-phenoxy)-2,2dimethylpentyl)-benzamide Derivatives as Novel Farnesoid X Receptor (FXR) Antagonist [J] . Nian Siyun, Yu Zhenpeng, Tan Xiangduan, Letters in drug design & discovery . 2018,第9期

机译：N-（5-（2,5-二甲基 - 苯氧基）-2,2二甲基戊基） - 苄酰胺衍生物作为新型法呢X受体（FXR）拮抗剂的合成及生物学评价
2. Synthesis and biological evaluations of chalcones, flavones and chromenes as farnesoid x receptor (FXR) antagonists [J] . Zhang Guoning, Liu Shuainan, Tan Wenjuan, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2017,第期

机译：Chalcones，黄酮和铬的合成和生物学评价为法呢X受体（FXR）拮抗剂
3. Design, Synthesis and Biological Evaluation of Novel N-(4-(2,2':5',2"-Terthiophen-5-yl)-2-methylbut-3-yn-2-yl) Benzamide Derivatives [J] . Youquan Zhu, Haili Zhang, Danyang Wang, 中国化学（英文版） . 2015,第002期

机译：新型N-（4-（2,2'：5'，2“-对噻吩基 -5-基）-2-甲基丁-3-yn-2-基）苯甲酰胺衍生物的设计，合成和生物评价
4. Synthesis of N-(2,3-dihydro-1-~14Cmethyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl)-benzamide and N-(2,3-dihydro-l-~14Cmethyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl) - N -~14C methyl-benzamide as novel carbon-14 labelled CCK Antagonists [C] . Gholamhossein Shirvani, Hojatollah Matloubi Nader Saemian International Conference on Isotopes (5ICI) . 2005

机译：N-（2,3-二氢-1- 〜14℃甲基-2-氧代-5-苯基-1H-1,4-苯并二氮哌己嘧啶-3-基-3-基（2,3-二氢）的合成-1- 〜14c甲基-2-氧代-5-苯基-1H-1,4-苯并二氮嘧啶-3-基） - N - 〜14C甲基 - 苯甲酰胺作为新型碳-14标记的CCK拮抗剂
5. Design, synthesis and biological evaluation of benzamide and phenyltetrazole derivatives with amide and urea linkers as BCRP inhibitors [D] . Gujarati, Nehaben A. 2017

机译：以酰胺和脲连接基作为BCRP抑制剂的苯甲酰胺和苯基四唑衍生物的设计，合成和生物学评估
6. Synthesis and Biological Evaluation of N-(5-(pyridin-2-yl)-134-thiadiazol-2-yl)benzamide Derivatives as Lipoxygenase Inhibitor with Potential Anticancer Activity [O] . Alireza Aliabadi, Ahmad Mohammadi-Farani, Sahar Roodabeh, 2017

机译：具有潜在抗癌活性的脂氧合酶抑制剂N-（5-（吡啶-2-基）-134-噻二唑-2-基）苯甲酰胺衍生物的合成及生物学评价
7. Synthesis and biological evaluations of chalcones, flavones and chromenes as farnesoid x receptor (FXR) antagonists [O] . Guoning Zhang, Shuainan Liu, Wenjuan Tan, 2017

机译：Chalcones，黄酮和铬的合成和生物学评价为法呢X受体（FXR）拮抗剂

Synthesis and Biological Evaluation of N-(5-(2,5-dimethyl-phenoxy)-2,2dimethylpentyl)-benzamide Derivatives as Novel Farnesoid X Receptor (FXR) Antagonist

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