新一代多巴胺能药物。5. 利用3-羟基-N1-苯基哌嗪多巴胺能模板的杂环生物电子等排体。
New generation dopaminergic agents. 5. Heterocyclic bioisosteres that exploit the 3-OH-N1-phenylpiperazine dopaminergic template.
作者信息
Mewshaw R E, Verwijs A, Shi X, McGaughey G B, Nelson J A, Mazandarani H, Brennan J A, Marquis K L, Coupet J, Andree T H
机构信息
Global Chemical Sciences, Wyeth-Ayerst Research Laboratory, Princeton, NJ 08543-8000, USA.
出版信息
Bioorg Med Chem Lett. 1998 Oct 6;8(19):2675-80. doi: 10.1016/s0960-894x(98)00474-0.
The synthesis of several bioisosteric analogs based on the 3-OH-N1-phenylpiperazine dopamine D2 agonist template (i.e., 4) is described. The indolone (5) and 2-CF3-benzimidazole (13) were observed to have excellent affinity for the D2 receptor. Several D4 selective compounds were also identified. Molecular modeling studies and a putative bioactive conformation are discussed.
描述了基于3-羟基-N1-苯基哌嗪多巴胺D2激动剂模板（即4）的几种生物电子等排体类似物的合成。观察到吲哚酮（5）和2-三氟甲基苯并咪唑（13）对D2受体具有优异的亲和力。还鉴定了几种D4选择性化合物。讨论了分子建模研究和推定的生物活性构象。
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