The search for novel TRPV1-antagonists: From carboxamides to benzimidazoles and indazolones

被引：61

作者：

Fletcher, SR ^{[1
]}

McIver, E ^{[1
]}

Lewis, S ^{[1
]}

Burkamp, F ^{[1
]}

Leech, C ^{[1
]}

Mason, G ^{[1
]}

Boyce, S ^{[1
]}

Morrison, D ^{[1
]}

Richards, G ^{[1
]}

Sutton, K ^{[1
]}

Jones, AB ^{[1
]}

机构：

[1] Merck Sharp & Dohme Ltd, Ctr Res Neurosci, Harlow CM20 2QR, Essex, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 11期

关键词：

TRPV-1; antagonists; indazolone; benzimidazole;

D O I：

10.1016/j.bmcl.2006.03.004

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Based on a series of diaryl amides the corresponding inverse amides have been found to be potent TRPV1 receptor antagonists. Benzimidazole and indazolone derivatives prepared retained good potency in vitro and indazolone 4a was identified as a novel TRPV1 receptor antagonist suitable for evaluating orally in animal models of analgesia. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：2872 / 2876

页数：5

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