Pyridinesulfonylureas and pyridinesulfonamides as selective bombesin receptor subtype-3 (BRS-3) agonists.
Pyridinesulfonylureas and pyridinesulfonamides as selective bombesin receptor subtype-3 (BRS-3) agonists.
复制标题
吡啶磺酰脲类和吡啶磺酰胺类作为选择性铃蟾肽受体亚型 3 (BRS-3) 激动剂。
DOI：
10.1016/j.bmcl.2011.02.011
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发表时间：
2011
影响因子：
2.7
通讯作者：
Lin,LinusS
中科院分区：
文献类型：
--
作者：
Lo,MichaelM-C;Chobanian,HarryR;Palyha,Oksana;Kan,Yanqing;Kelly,TheresaM;Guan,Xiao-Ming;Reitman,MarcL;Dragovic,Jasminka;Lyons,KathrynA;Nargund,RaviP;Lin,LinusS
蛙皮素受体亚型-3（BRS-3）是属于蛙皮素样受体亚家族的孤儿G蛋白偶联受体。BRS-3与肥胖和糖尿病的发展有关。我们在这里报告的小分子激动剂，是基于4-（烷氨基）吡啶-3-磺酰胺核心。我们描述了2a的发现，其具有中等纳摩尔的效力，对人BRS-3相对于其他铃蟾肽样受体的选择性，以及良好的生物利用度。
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.