Heteroatom-linked indanylpyrazines are corticotropin releasing factor type-1 receptor antagonists
Heteroatom-linked indanylpyrazines are corticotropin releasing factor type-1 receptor antagonists
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DOI：
10.1016/j.bmcl.2007.09.008
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发表时间：
2007-11-15
影响因子：
2.7
通讯作者：
Fitzgerald, Lawrence W.
中科院分区：
文献类型：
--
作者：
Corbett, Jeffrey W.;Rauckhorst, Mark R.;Fitzgerald, Lawrence W.
低纳摩尔促肾上腺皮质激素释放因子1型（CRF 1）受体拮抗剂含有独特的茚满胺从杂原子连接的吡嗪化学型。最有效的茚满基吡嗪的Ki = 11 +/- 1 nM。通过铜催化的吡啶酮与溴吡嗪或碘吡嗪的偶联反应制备了氧连接的吡嗪衍生物。(C)2007爱思唯尔有限公司保留所有权利。
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.