新型系列促黑素细胞激素（MCH）受体拮抗剂的构效关系
Structure-activity relationships of a novel series of melanin-concentrating hormone (MCH) receptor antagonists.
作者信息
Arienzo Rosa, Clark David E, Cramp Sue, Daly Stephen, Dyke Hazel J, Lockey Peter, Norman Dennis, Roach Alan G, Stuttle Keith, Tomlinson Maxine, Wong Melanie, Wren Stephen P
机构信息
Argenta Discovery Limited, 8/9 Spire Green Centre, Flex Meadow, Harlow, Essex CM19 5TR, UK.
出版信息
Bioorg Med Chem Lett. 2004 Aug 2;14(15):4099-102. doi: 10.1016/j.bmcl.2004.05.051.
A new series of 2-aminoquinolines has been identified as antagonists of the melanin concentrating hormone receptor (MCH-1R). Syntheses and structure-activity relationships are described leading to a compound having low nanomolar activity against the receptor and demonstrating functional antagonism. Studies also showed that some of the compounds were selective against a range of other G protein-coupled receptors.
一系列新的2-氨基喹啉已被鉴定为黑色素浓缩激素受体（MCH-1R）的拮抗剂。本文描述了其合成方法及构效关系，最终得到了一种对该受体具有低纳摩尔活性并表现出功能拮抗作用的化合物。研究还表明，其中一些化合物对一系列其他G蛋白偶联受体具有选择性。
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