Arylpiperazine-containing pyrimidine 4-carboxamide derivatives targeting serotonin 5-HT2A, 5-HT2C, and the serotonin transporter as a potential antidepressant

被引：37

作者：

Kim, Jong Yup ^{[1
,2
]}

Kim, Deukjoon ^{[1
]}

Kang, Suk Youn ^{[2
]}

Park, Woo-Kyu ^{[3
]}

Kim, Hyun Jung ^{[2
]}

Jung, Myung Eun ^{[2
]}

Son, Eun-Jung ^{[2
]}

Pae, Ae Nim ^{[4
]}

Kim, Jeongmin ^{[2
]}

Lee, Jinhwa ^{[2
]}

机构：

[1] Seoul Natl Univ, Pharmaceut Sci Res Inst, Coll Pharm, Seoul 151742, South Korea

[2] Green Cross Co, Res Ctr, Yongin 446770, South Korea

[3] Korea Res Inst Chem Technol, Pharmacol Res Ctr, Taejon 305343, South Korea

[4] Korea Inst Sci & Technol, Biochem Res Ctr, Seoul 136791, South Korea

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 22期

关键词：

Antidepressant; Serotonin; Piperazine; Pyrimidine; RECEPTOR ANTAGONIST; REUPTAKE INHIBITORS; BIPOLAR DISORDER; NEUROPSYCHOLOGY; NEFAZODONE;

D O I：

10.1016/j.bmcl.2010.09.081

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Pyrimidine usually has good pharmacokinetic properties as a drug substance and considerable efforts have been devoted to develop pyrimidine derivatives into drug candidates. Arylpiperazine-containing pyrimidine 4-carboxamide derivatives were synthesized and evaluated for binding to serotonin receptors and transporter. Pyrimidine derivatives showed good antidepressant activity in FST (forced swimming test) animal model and also displayed no appreciable inhibitory activity against hERG channel blocking assay. Herein SAR studies of pyrimidine derivatives targeting serotonin receptors and transporter will be disclosed. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：6439 / 6442

页数：4

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