Synthesis of BMS-309403-Related Compounds, Including [14C]BMS-309403, a Radioligand for Adipocyte Fatty Acid Binding Protein
Synthesis of BMS-309403-Related Compounds, Including [14C]BMS-309403, a Radioligand for Adipocyte Fatty Acid Binding Protein
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DOI：
10.1248/cpb.60.164
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发表时间：
2012-01-01
影响因子：
1.7
通讯作者：
Miyachi, Hiroyuki
中科院分区：
文献类型：
--
作者：
Okada, Toshihiko;Hiromura, Makoto;Miyachi, Hiroyuki
脂肪细胞脂肪酸结合蛋白（A-FABP; FABP 4）主要在巨噬细胞和脂肪组织中表达，调节脂肪酸储存和脂解，也是炎症的重要介质。在这里，我们报告了C-14标记的2-[2 '-（5-乙基-3，4-二苯基-1H-吡唑-1-基）联苯-3-基氧基]乙酸（BMS 309403）的合成，该化合物是一种有效的选择性小分子FABP 4抑制剂，作为研究FABP 4在炎症和代谢疾病中作用的化学工具。本文还报道了几种BMS衍生物抑制FABP 4的构效关系。
Adipocyte fatty acid binding protein (A-FABP; FABP4), which is predominantly expressed in macrophages and adipose tissue, regulates fatty acid storage and lipolysis, and is also an important mediator of inflammation. Here, we report a synthesis of C-14-labeled 2-[2'-(5-ethyl-3,4-diphenyl-1H-pyrazol-1-yl)biphenyl-3-yloxy]acetic acid (BMS309403), a potent and selective small-molecular FABP4 inhibitor, as a chemical tool for investigating the roles of FABP4 in inflammatory and metabolic disorders. The structure activity relationship of several BMS derivatives for inhibition of FABP4 is also reported.