Heteroatom-linked indanylpyrazines are corticotropin releasing factor type-1 receptor antagonists

被引：41

作者：

Corbett, Jeffrey W. ^{[1
]}

Rauckhorst, Mark R. ^{[1
]}

Qian, Fang ^{[1
]}

Hoffman, Robert L. ^{[1
]}

Knauer, Christopher S. ^{[1
]}

Fitzgerald, Lawrence W. ^{[1
]}

机构：

[1] Pfizer Global Res & Dev, Groton, CT 06340 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 22期

关键词：

corticotropin releasing factor type-1 antagonist; CRF1; corticotropin releasing hormone type-1; CRH1; pyrazine; copper-mediated coupling;

D O I：

10.1016/j.bmcl.2007.09.008

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Low nanomolar corticotropin releasing factor type-1 (CRF1) receptor antagonists containing unique indanylamines were identified from the heteroatom-linked pyrazine chemotype. The most potent indanylpyrazine had a K-i = 11 +/- 1 nM. The oxygen-linked pyrazinyl derivatives were prepared through a copper-catalyzed coupling of a pyridinone to a bromo- or iodopyrazine. (C) 2007 Elsevier Ltd. All rights reserved.

引用

页码：6250 / 6256

页数：7

共 23 条

[1] Cu-catalyzed N- and O-arylation of 2-, 3-, and 4-hydroxypyridines and hydroxyquinolines [J].