Synthesis and biological activity of oxo-7H-benzo[e]perimidine-4-carboxylic acid derivatives as potent, nonpeptide corticotropin releasing factor (CRF) receptor antagonists

被引：37

作者：

Luthin, DR ^{[1
]}

Rabinovich, AK ^{[1
]}

Bhumralkar, DR ^{[1
]}

Youngblood, KL ^{[1
]}

Bychowski, RA ^{[1
]}

Dhanoa, DS ^{[1
]}

May, JM ^{[1
]}

机构：

[1] Alanex Corp, San Diego, CA 92121 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 05期

关键词：

D O I：

10.1016/S0960-894X(99)00075-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of derivatives of oxo-7H-benzo[e]perimidine-4-carboxylic acid (I) potently displaced radioligand binding of I-125-CRF to both CRF1 and CRF2 receptors. The members of this series antagonized CRF-stimulated cAMP formation and CRF-stimulated corticotropin release from rat pituitary in vivo. These are the first nonpeptide antagonists to show activity at both CRF1 and CRF2 receptors. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：765 / 770

页数：6

共 6 条

[1]

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[2]

DESOUZA EB, 1995, ANNU REP MED CHEM, V30, P21

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