Discovery of diacylphloroglucinols as a new class of GPR40 (FFAR1) agonists.

Bharate SB; Rodge A; Joshi RK; Kaur J; Srinivasan S; Kumar SS; Kulkarni-Almeida A; Balachandran S; Balakrishnan A; Vishwakarma RA

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Discovery of diacylphloroglucinols as a new class of GPR40 (FFAR1) agonists.

机译：发现二酰基间苯二酚作为一种新的GPR40（FFAR1）激动剂。

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In this letter, we report discovery of diacylphloroglucinol compounds as a new class of GPR40 (FFAR1) agonists. Several diacylphloroglucinols with varying length of acyl functionality and substitution on aromatic hydroxyls were synthesized and evaluated for GPR40 agonism using functional calcium-flux assay. Out of 17 compounds evaluated, 14, 17, 19 and 25 exhibited good GPR40 agonistic activity with EC(50) values ranging from 0.07 to 8 microM (pEC(50) 7.12-5.09), respectively, with maximal agonistic response of 84-102%.

机译：在这封信中，我们报告了发现二酰基间苯三酚化合物作为新型GPR40（FFAR1）激动剂的发现。合成了几种具有不同长度的酰基官能团并在芳族羟基上取代的二酰基间苯二酚，并使用功能性钙通量测定法评估了GPR40激动作用。在评估的17种化合物中，14、17、19和25表现出良好的GPR40激动活性，EC（50）值分别为0.07至8 microM（pEC（50）7.12-5.09），最大激动反应为84-102 ％。

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《Bioorganic and Medicinal Chemistry Letters》 |2008年第24期|共5页
作者
Bharate SB; Rodge A; Joshi RK; Kaur J; Srinivasan S; Kumar SS; Kulkarni-Almeida A; Balachandran S; Balakrishnan A; Vishwakarma RA;
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正文语种 eng
中图分类药学;生物化学;
关键词
agonists; Length; assay; Calcium; 钙;

机译：激动剂;长度;测定;钙;钙;

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1. Discovery of diacylphloroglucinols as a new class of GPR40 (FFAR1) agonists. [J] . Bharate SB, Rodge A, Joshi RK, Bioorganic and Medicinal Chemistry Letters . 2008,第24期

机译：发现二酰基间苯二酚作为一种新的GPR40（FFAR1）激动剂。
2. Discovery of 5-aryloxy-2,4-thiazolidinediones as potent GPR40 agonists. [J] . Zhou C, Tang C, Chang Bioorganic and Medicinal Chemistry Letters . 2010,第3期

机译：发现了5-芳氧基-2,4-噻唑烷二酮类作为有效的GPR40激动剂。
3. Discovery of a novel class of 2-mercaptohexanoic acid derivatives as highly active PPARalpha agonists. [J] . Zettl H, Steri R, Lammerhofer M Bioorganic and Medicinal Chemistry Letters . 2009,第15期

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机译：效力和选择性肽V1A受体激动剂的合成与体外药理学谱。
5. Photoemission studies of a new topological insulator class: Experimental discovery of the bismuth-X3 topological insulator class. [D] . Xia, YuQi. 2010

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6. Molecular dynamics-guided discovery of an ago-allosteric modulator for GPR40/FFAR1 [O] . Michael Lückmann, Mette Trauelsen, Marie A. Bentsen, 2019

机译：分子动力学指导的GPR40 / FFAR1变构调节剂的发现
7. Molecular dynamics-guided discovery of an ago-allosteric modulator for GPR40/FFAR1 [O] . Michael Lückmann, Mette Trauelsen, Marie A. Bentsen, 2019

机译：分子动力学引导的发现对GPR40 / FFAR1的颠振调制器

Discovery of diacylphloroglucinols as a new class of GPR40 (FFAR1) agonists.

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