Chromenones as potent bradykinin B1 antagonists

被引：10

作者：

Bryan, Marian C. ^{[1
]}

Biswas, Kaustav ^{[1
]}

Peterkin, Tanya A. N. ^{[1
]}

Rzasa, Robert M. ^{[1
]}

Arik, Leyla ^{[3
]}

Lehto, Sonya G. ^{[3
]}

Sun, Hong ^{[3
]}

Hsieh, Feng-Yin ^{[2
]}

Xu, Cen ^{[3
]}

Fremeau, Robert T. ^{[3
]}

Allen, Jennifer R. ^{[1
]}

机构：

[1] Amgen Inc, Dept Chem Res & Discovery, Thousand Oaks, CA 91320 USA

[2] Amgen Inc, Dept Pharmacokinet & Drug Metab, Thousand Oaks, CA 91320 USA

[3] Amgen Inc, Dept Neurosci Res, Thousand Oaks, CA 91320 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 01期

关键词：

Bradykinin B1 receptor; Chromenone; Inflammatory pain; KALLIKREIN-KININ SYSTEM; RECEPTOR ANTAGONISTS; THERAPEUTIC AGENTS; PAIN;

D O I：

10.1016/j.bmcl.2011.10.068

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of fused 6,6-bicyclic chromenones was investigated for activity against the bradykinin B1 receptor. SAR studies based on a pharmacophore model revealed compounds with high affinity for both human and rabbit B1. These compounds demonstrated favorable pharmacokinetic properties and 5-chlorochromenone 15 was efficacious in a carrageenan-induced mechanical hyperalgesia model for chronic pain. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：619 / 622

页数：4

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