Discovery of diacylphloroglucinols as a new class of GPR40 (FFAR1) agonists
Discovery of diacylphloroglucinols as a new class of GPR40 (FFAR1) agonists
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DOI：
10.1016/j.bmcl.2008.10.085
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发表时间：
2008-12-15
影响因子：
2.7
通讯作者：
Vishwakarma, Ram A.
中科院分区：
文献类型：
--
作者：
Bharate, Sandip B.;Rodge, Atish;Vishwakarma, Ram A.
在这封信中，我们报告了作为一类新的GPR 40（FFAR 1）激动剂的二酰基间苯三酚化合物的发现。几个二酰基间苯三酚与不同长度的酰基功能和取代的芳香族羟基的合成和评估GPR 40激动剂使用功能性钙通量测定。在评价的17种化合物中，14、17、19和25种表现出良好的GPR 40激动活性，EC（50）值分别为0.07 - 8 μ M（pEC（50）7.12-5.09），最大激动反应为84- 102%。(C)2008爱思唯尔有限公司保留所有权利。
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 mu M (pEC(50) 7.12-5.09), respectively, with maximal agonistic response of 84-102%. (C) 2008 Elsevier Ltd. All rights reserved.