促黑素受体1拮抗剂SB-568849的强效且稳定的构象受限类似物的发现。
Discovery of potent and stable conformationally constrained analogues of the MCH R1 antagonist SB-568849.
作者信息
Witty David R, Bateson John, Hervieu Guillaume J, Al-Barazanji Kamal, Jeffrey Phillip, Hamprecht Dieter, Haynes Andrea, Johnson Christopher N, Muir Alison I, O'Hanlon Peter J, Stemp Geoffrey, Stevens Alex J, Thewlis Kevin, Winborn Kim Y
机构信息
GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK.
出版信息
Bioorg Med Chem Lett. 2006 Sep 15;16(18):4872-8. doi: 10.1016/j.bmcl.2006.06.061. Epub 2006 Jul 12.
A strategy of systematically targeting more rigid analogues of the known MCH R1 receptor antagonist, SB-568849, serendipitously uncovered a binding mode accessible to N-aryl-phthalimide ligands. Optimisation to improve the stability of this compound class led to the discovery of novel N-aryl-quinazolinones, benzotriazinones and thienopyrimidinones as selective ligands with good affinity for human melanin-concentrating hormone receptor 1.
一种系统地靶向已知的促黑素细胞激素受体1（MCH R1）拮抗剂SB-568849更刚性类似物的策略，意外地发现了一种N-芳基邻苯二甲酰亚胺配体可及的结合模式。为提高这类化合物的稳定性而进行的优化，导致发现了新型的N-芳基喹唑啉酮、苯并三嗪酮和噻吩并嘧啶酮作为对人促黑素细胞激素受体1具有良好亲和力的选择性配体。
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