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Feasible Synthesis of Antagonist of GPR40 by Constructing 2-Thiouracil Ring viaAcid Mediated Cyclization.通过酸介导环化构建2-硫尿嘧啶环实现GPR40拮抗剂的可行性合成
Heterocycles. 2011 May 1;83(5):1145-1151. doi: 10.3987/COM-11-12175.
2
Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules.通过脂肪酸受体GPR40对MIN6细胞中胰岛素分泌的药理学调节：激动剂和拮抗剂小分子的鉴定
Br J Pharmacol. 2006 Jul;148(5):619-28. doi: 10.1038/sj.bjp.0706770. Epub 2006 May 15.
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Chronic activation of GPR40 does not negatively impact upon BRIN-BD11 pancreatic β-cell physiology and function.GPR40的慢性激活对BRIN-BD11胰腺β细胞的生理和功能没有负面影响。
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Differential free fatty acid receptor-1 (FFAR1/GPR40) signalling is associated with gene expression or gelatinase granule release in bovine neutrophils.差异游离脂肪酸受体1（FFAR1/GPR40）信号传导与牛中性粒细胞中的基因表达或明胶酶颗粒释放有关。
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Involvement of G-Protein-Coupled Receptor 40 in the Inhibitory Effects of Docosahexaenoic Acid on SREBP1-Mediated Lipogenic Enzyme Expression in Primary Hepatocytes.二十二碳六烯酸通过 G 蛋白偶联受体 40 抑制原代肝细胞固醇调节元件结合蛋白 1 介导的脂肪生成酶表达。
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The involvement of free fatty acid-GPR40/FFAR1 signaling in chronic social defeat stress-induced pain prolongation in C57BL/6J male mice.游离脂肪酸-GPR40/FFAR1 信号通路参与慢性社会挫败应激诱导的 C57BL/6J 雄性小鼠痛觉敏感延长。
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Diverse effects of G-protein-coupled free fatty acid receptors on the regulation of cellular functions in lung cancer cells.G蛋白偶联游离脂肪酸受体对肺癌细胞中细胞功能调节的多种作用。
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Hypothalamic GPR40 signaling activated by free long chain fatty acids suppresses CFA-induced inflammatory chronic pain.游离长链脂肪酸激活的下丘脑GPR40信号传导可抑制弗氏完全佐剂诱导的炎性慢性疼痛。
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Activation of GPR40 as a therapeutic target for the treatment of type 2 diabetes.GPR40 的激活作为治疗 2 型糖尿病的治疗靶点。
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n-Butyl 5-Chloro-2-pyrimidoxyacetate--a Plant Growth Regulator Analog.
Science. 1958 Aug 29;128(3322):480. doi: 10.1126/science.128.3322.480.
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Synthesis and evaluation of a new series of substituted acyl(thio)urea and thiadiazolo [2,3-a] pyrimidine derivatives as potent inhibitors of influenza virus neuraminidase.新型取代酰基（硫代）脲和噻二唑并[2,3-a]嘧啶衍生物作为流感病毒神经氨酸酶强效抑制剂的合成与评价
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Synthesis of functionalized diarylmethanes via a copper-catalyzed cross-coupling of arylmagnesium reagents with benzylic phosphates.通过铜催化芳基镁试剂与苄基磷酸酯的交叉偶联反应合成功能化二芳基甲烷。
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Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules.通过脂肪酸受体GPR40对MIN6细胞中胰岛素分泌的药理学调节：激动剂和拮抗剂小分子的鉴定
Br J Pharmacol. 2006 Jul;148(5):619-28. doi: 10.1038/sj.bjp.0706770. Epub 2006 May 15.
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The FFA receptor GPR40 links hyperinsulinemia, hepatic steatosis, and impaired glucose homeostasis in mouse.游离脂肪酸（FFA）受体GPR40与小鼠的高胰岛素血症、肝脂肪变性及葡萄糖稳态受损相关。
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Total synthesis of pinnamine and anatoxin-a via a common intermediate. A caveat on the anatoxin-a endgame.通过一个共同中间体全合成海葵胺和类毒素-a。关于类毒素-a合成最后步骤的一个提醒。
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Free fatty acids regulate insulin secretion from pancreatic beta cells through GPR40.游离脂肪酸通过GPR40调节胰腺β细胞的胰岛素分泌。
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通过酸介导环化构建2-硫尿嘧啶环实现GPR40拮抗剂的可行性合成

Feasible Synthesis of Antagonist of GPR40 by Constructing 2-Thiouracil Ring viaAcid Mediated Cyclization.

作者信息

Zhao Yongfeng, Song Yang, Shen Xiulin, Liao Jiayu

机构信息

Department of Bioengineering, Bourns College of Engineering, University of California-Riverside, Riverside, CA 92507, USA.

出版信息

Heterocycles. 2011 May 1;83(5):1145-1151. doi: 10.3987/COM-11-12175.

DOI:10.3987/COM-11-12175
PMID:21776181
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3137925/
Abstract

GW1100 is an antagonist of GPR40 identified by high throughput screening recently. The synthesis of GW1100 has been developed. The key step involves cyclization of the 2-thiouracil heterocycle under acidic condition at room temperature.

摘要

GW1100是最近通过高通量筛选鉴定出的GPR40拮抗剂。GW1100的合成方法已经开发出来。关键步骤包括在室温酸性条件下2-硫脲杂环的环化反应。