Pharmacophore-based discovery, synthesis, and biological evaluation of 4-phenyl-1-arylalkyl piperidines as dopamine transporter inhibitors

被引：24

作者：

Sakamuri, S

Enyedy, IJ

Kozikowski, AP

Zaman, WA

Johnson, KM

Wang, SM

机构：

[1] Georgetown Univ, Med Ctr, Drug Discovery Program, Washington, DC 20007 USA

[2] Georgetown Univ, Med Ctr, Dept Neurol, Washington, DC 20007 USA

[3] Georgetown Univ, Med Ctr, Dept Oncol, Washington, DC 20007 USA

[4] Georgetown Univ, Med Ctr, Dept Neurosci, Washington, DC 20007 USA

[5] Univ Texas, Med Branch, Dept Pharmacol & Toxicol, Galveston, TX 77555 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 04期

关键词：

D O I：

10.1016/S0960-894X(00)00703-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Pharmacophore-based discovery, synthesis, and structure-activity relationship (SAR) of a series of 4-phenyl-1-arylalkyl piperidines are disclosed. These compounds have been evaluated for their ability to inhibit reuptake of dopamine (DA) into striatal nerve endings (synaptosomes). The lead compound 5 and the most potent analogue 43 were found to have significant functional antagonism. (C) 2001 Elsevier Science Ltd. All rights reserved.

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页码：495 / 500

页数：6

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