2,3-diaminopyridine bradykinin B1 receptor antagonists

被引：42

作者：

Kuduk, SD

Ng, C

Feng, DM

Wai, JMC

Chang, RSL

Harrell, CM

Murphy, KL

Ransom, RW

Reiss, D

Ivarsson, M

Mason, G

Boyce, S

Tang, CY

Prueksaritanont, T

Freidinger, RM

Pettibone, DJ

Bock, MG

机构：

[1] Merck Res Labs, Dept Med Chem, West Point, PA 19486 USA

[2] Merck Res Labs, Dept Drug Metab, West Point, PA 19486 USA

[3] Merck Res Labs, Dept Neurosci Drug Discovery, West Point, PA 19486 USA

[4] Merck Res Labs, Neurosci Res Ctr, Harlow CM20 2QR, Essex, England

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2004年 / 47卷 / 26期

关键词：

D O I：

10.1021/jm049394l

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Bradykinin B-1 receptor antagonists embody a potentially novel approach for the treatment of chronic pain and inflammation. A series of 2,3-diaminopyridine B-1 antagonists was optimized to have sub-nanomolar affinity and good pharmacokinetic properties. Lead compounds were shown to exhibit good efficacy in rabbit in vivo models of pain and inflammation.

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收藏

页码：6439 / 6442

页数：4

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