1,3-dihydro-2,1,3-benzothiadiazol-2,2-diones and 3,4-dihydro-1H-2,1,3-benzothidiazin-2,2-diones as ligands for the NOP receptor

被引：13

作者：

Goehring, RR ^{[1
]}

Whitehead, JFW ^{[1
]}

Brown, K ^{[1
]}

Islam, K ^{[1
]}

Xin, W ^{[1
]}

Zhou, XM ^{[1
]}

Chen, ZM ^{[1
]}

Valenzano, KJ ^{[1
]}

Miller, WS ^{[1
]}

Shen, S ^{[1
]}

Kyle, DJ ^{[1
]}

机构：

[1] Purdue Pharma LP, Discovery Res, Cranbury, NJ 08512 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 20期

关键词：

D O I：

10.1016/j.bmcl.2004.08.001

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 1,3-dihydro-2,1,3-benzothiadiazol-2,2-diones (1) and 3,4-dihydro-1H-2,1,3-benzothidiazin-2,2-diones (II) were prepared. While the five-member ring series (I) did not show good affinity for opioid receptors, the six-member ring series (II) exhibited extremely high affinity and selectivity for the NOP receptor and showed full agonist activity, as determined by stimulation of GTPgamma[S-35] binding. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：5045 / 5050

页数：6

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