Identification of a subtype selective human PPARα agonist through parallel-array synthesis
Identification of a subtype selective human PPARα agonist through parallel-array synthesis
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DOI：
10.1016/s0960-894x(01)00188-3
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发表时间：
2001-05-07
影响因子：
2.7
通讯作者：
Willson, TM
中科院分区：
文献类型：
--
作者：
Brown, PJ;Stuart, LW;Willson, TM
使用固相平行阵列合成，合成了一系列脲取代的硫代异丁酸，并测定其对人PPAR亚型的活性。GW7647（3）被鉴定为一种有效的人PPAR α激动剂，其选择性是PPAR γ和PPAR δ的200倍，在血脂异常动物模型中具有有效的降脂活性。GW7647（3）将是研究人类细胞和动物疾病模型中PPAR α生物学的有价值的化学工具。(C)2001 Elsevier Science Ltd.保留所有权利。
Using solid-phase, parallel-array synthesis, a series of urea-substituted thioisobutyric acids was synthesized and assayed for activity on the human PPAR subtypes. GW7647 (3) was identified as a potent human PPAR alpha agonist with similar to 200-fold selectivity over PPAR gamma and PPAR delta, and potent lipid-lowering activity in animal models of dyslipidemia. GW7647 (3) will be a valuable chemical tool for studying the biology of PPAR alpha in human cells and animal models of disease. (C) 2001 Elsevier Science Ltd. Ail rights reserved.