Design, synthesis and evaluation of a novel cyclohexanamine class of neuropeptide Y Y1 receptor antagonists

被引：11

作者：

Cho, Kaimei ^{[1
]}

Ando, Makoto ^{[1
]}

Kobayashi, Kensuke ^{[1
]}

Miyazoe, Hiroshi ^{[1
]}

Tsujino, Toshiaki ^{[1
]}

Ito, Sayaka ^{[1
]}

Suzuki, Tomoki ^{[1
]}

Tanaka, Takeshi ^{[1
]}

Tokita, Shigeru ^{[1
]}

Sato, Nagaaki ^{[1
]}

机构：

[1] Banyu Pharmaceut Co Ltd, Merck Res Labs, Tsukuba Res Inst, Tsukuba, Ibaraki 3002611, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 16期

关键词：

NPY Y1 receptor antagonist; Cyclohexanamine; hERG K(+) channel; Serotonin transporter; SEROTONIN TRANSPORTER; PEPTIDE-YY; OBESITY; POTENT; NPYY1;

D O I：

10.1016/j.bmcl.2009.06.050

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of cyclohexanamine derivatives was designed and synthesized as potent and selective human neuropeptide Y Y1 receptor antagonists. Modification of high-throughput screening hit compound 1 resulted in the identification of compound 3i, which displays potent Y1 activity and good selectivity towards hERG K(+) channel and serotonin transporter. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：4781 / 4785

页数：5

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