吡啶磺酰脲类和吡啶磺酰胺类作为选择性脑肠肽受体亚型-3（BRS-3）激动剂。
Pyridinesulfonylureas and pyridinesulfonamides as selective bombesin receptor subtype-3 (BRS-3) agonists.
机构信息
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.
出版信息
Bioorg Med Chem Lett. 2011 Apr 1;21(7):2040-3. doi: 10.1016/j.bmcl.2011.02.011. Epub 2011 Feb 25.
Bombesin receptor subtype-3 (BRS-3) is an orphan G-protein coupled receptor belonging to the subfamily of bombesin-like receptors. BRS-3 is implicated in the development of obesity and diabetes. We report here small-molecule agonists that are based on a 4-(alkylamino)pyridine-3-sulfonamide core. We describe the discovery of 2a, which has mid-nanomolar potency, selectivity for human BRS-3 versus the other bombesin-like receptors, and good bioavailability.
蛙皮素受体亚型-3（BRS-3）是一种孤儿 G 蛋白偶联受体，属于蛙皮素样受体亚家族。BRS-3 与肥胖和糖尿病的发展有关。我们在此报告了基于 4-（烷基氨基）吡啶-3-磺酰胺核心的小分子激动剂。我们描述了 2a 的发现，它具有中纳摩尔效力，对人 BRS-3 相对于其他蛙皮素样受体的选择性，以及良好的生物利用度。
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