对多巴胺D4受体具有高亲和力的氮杂吲哚衍生物：合成、配体结合研究及分子静电势图比较
Azaindole derivatives with high affinity for the dopamine D4 receptor: synthesis, ligand binding studies and comparison of molecular electrostatic potential maps.
作者信息
Löber S, Hübner H, Gmeiner P
机构信息
Institut für Pharmazie und Lebensmittelchemie, Universität Erlangen-Nürnberg, Germany.
出版信息
Bioorg Med Chem Lett. 1999 Jan 4;9(1):97-102. doi: 10.1016/s0960-894x(98)00692-1.
PMID:9990464
Abstract
Piperazinylmethyl substituted pyrazolo[1,5-a]pyridines and related heterocycles were synthesized and found to recognize selectively the dopamine D4 receptor. For the most potent derivative 10d a Ki value of 2.0 nM was observed. SAR studies including the comparison of molecular isopotential surfaces were performed.
摘要
合成了哌嗪基甲基取代的吡唑并[1,5 - a]吡啶及相关杂环化合物，发现它们能选择性识别多巴胺D4受体。对于最有效的衍生物10d，观察到其Ki值为2.0 nM。进行了包括分子等势面比较在内的构效关系研究。
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