Shearer Barry G, Chao Esther Y, Uehling David E, Deaton David N, Cowan Conrad, Sherman Bryan W, Milliken Tula, Faison Walter, Brown Kathleen, Adkison Kimberly K, Lee Frank
Department of Medicinal Chemistry, GlaxoSmithKline, Research Triangle Park, NC 27709, USA.
Bioorg Med Chem Lett. 2007 Aug 15;17(16):4670-7. doi: 10.1016/j.bmcl.2007.05.069. Epub 2007 May 25.
The design, synthesis, and SAR of a novel series of heterobiaryl phenethanolamine beta3 adrenergic receptor agonists are described. The furan analogue 49 was shown to elicit a significant dose-dependent lowering of plasma glucose in a rodent model of type 2 diabetes.
描述了一系列新型杂芳基苯乙醇胺β3肾上腺素能受体激动剂的设计、合成及构效关系。呋喃类似物49在2型糖尿病啮齿动物模型中显示出显著的剂量依赖性降低血糖作用。