一类新型的哒嗪系列GABAA α5配体。
A new pyridazine series of GABAA alpha5 ligands.
作者信息
van Niel Monique B, Wilson Kevin, Adkins Charles H, Atack John R, Castro José L, Clarke Dawn E, Fletcher Stephen, Gerhard Ute, Mackey Mark M, Malpas Sallie, Maubach Karen, Newman Robert, O'Connor Desmond, Pillai Gopalan V, Simpson Peter B, Thomas Steven R, MacLeod Angus M
机构信息
Department of Medicinal Chemistry, Merck Sharp & Dohme Research Laboratories, Terlings Park, Eastwick Road, Harlow, Essex, CM20 2QR, United Kingdom.
出版信息
J Med Chem. 2005 Sep 22;48(19):6004-11. doi: 10.1021/jm050249x.
Screening of the Merck compound collection identified 6 as an unusually simple, low molecular weight hit with moderate affinity for GABAA receptors. The structural novelty of 6, compared to our advanced series of GABAA alpha5 inverse agonists, made it an attractive molecule for further exploration. This paper will describe the evolution of 6 into a new series of ligands with nanomolar affinity and functional selectivity for GABAA alpha5 receptor subtypes.
对默克化合物库的筛选确定了6号化合物是一种异常简单的低分子量活性分子，对GABAA受体具有中等亲和力。与我们先进的GABAA α5反向激动剂系列相比，6号化合物的结构新颖性使其成为一个有吸引力的进一步探索的分子。本文将描述6号化合物演变成一系列对GABAA α5受体亚型具有纳摩尔亲和力和功能选择性的新配体的过程。
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