Rational design and synthesis of novel 2,5-disubstituted cis- and trans-piperidine derivatives exhibiting differential activity for the dopamine transporter
Rational design and synthesis of novel 2,5-disubstituted cis- and trans-piperidine derivatives exhibiting differential activity for the dopamine transporter
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DOI：
10.1016/s0960-894x(01)00443-7
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发表时间：
2001-09-03
影响因子：
2.7
通讯作者：
Reith, MEA
中科院分区：
文献类型：
--
作者：
Dutta, AK;Davis, MC;Reith, MEA
在此，我们报告了顺式和反式异构体形式的新型2,5-二取代哌啶衍生物的合理设计和合成。在这两种异构体中，顺式异构体 7a 被发现对多巴胺转运蛋白表现出最有效的活性和选择性。这些新型衍生物代表了 GBR 化合物哌啶类似物的构象受限版本。 (C) 2001 Elsevier Science Ltd. 保留所有权利。
Herein, we report the rational design and synthesis of novel 2,5-disubstituted piperidine derivatives in the cis and trans isomeric forms. Out of these two isomers, the cis-isomer, 7a, Was found to exhibit the most potent activity and selectivity for the dopamine transporter. These novel derivatives represent conformationally constrained version of piperidine analogue of GBR compounds. (C) 2001 Elsevier Science Ltd. All rights reserved.