New oxadiazolidinedione derivatives as potent and selective human β3 agonists

被引：21

作者：

Hu, BH ^{[1
]}

Malamas, M

Ellingboe, J

Largis, E

Han, S

Mulvey, R

Tillett, J

机构：

[1] Wyeth Ayerst Res, Pearl River, NY 10965 USA

[2] Wyeth Ayerst Res, Princeton, NJ 08543 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 08期

关键词：

D O I：

10.1016/S0960-894X(01)00147-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

As part of our investigation into the development of potent and selective human beta (3) agonists, a series of thiazolidinedione analogues was prepared and evaluated For their biological activity on the human beta (3)-adrenergic receptor. The oxadiazolidinedione derivative 17 was found to be the most potent and selective compound in this study, with an EC50 value of 0.02 muM at the beta (3) receptor. 259-fold selectivity over the beta (1) receptor. and 745-fold selectivity over the beta (2) receptor. (C) 2001 Elsevier Science Ltd. All rights reserved.

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页码：981 / 984

页数：4

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