Discovery of tetralin carboxamide growth hormone secretagogue receptor antagonists via scaffold manipulation

被引：30

作者：

Zhao, HY ^{[1
]}

Xin, ZL ^{[1
]}

Liu, G ^{[1
]}

Schaefer, VG ^{[1
]}

Falls, HD ^{[1
]}

Kaszubska, W ^{[1
]}

Collins, CA ^{[1
]}

Sham, HL ^{[1
]}

机构：

[1] Abbott Labs, Metab Dis Res, Global Pharmaceut Res & Dev, Abbott Pk, IL 60064 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2004年 / 47卷 / 27期

关键词：

D O I：

10.1021/jm0491750

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A case study of rational design of an efficient, specific, and proprietary molecular scaffold based on the structure-activity relationship (SAR) information on a screening hit is described. Potent, selective, and orally bioavailable tetralin carboxamide growth hormone secretagogue receptor (GHS-R) antagonists were discovered. Union of rational design and high throughput synthesis provided a quick access to high quality chemical leads.

引用

页码：6655 / 6657

页数：3

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