Novel small molecule bradykinin B1 receptor antagonists. Part 2: 5-membered diaminoheterocycles.

Gunther Zischinsky,Roland Stragies,Marco Schaudt,Jochen R Pfeifer,Christoph Gibson,Elsa Locardi,Dirk Scharn,Uwe Richter,Holger Kalkhof,Klaus Dinkel,Karsten Schnatbaum

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS（2010）

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摘要

Efforts to find new bradykinin B-1 receptor antagonists identified 2-aminobenzimidazole as a novel core. Subsequent transformation into five-membered diaminoheterocycle derivatives and their synthesis and SAR is described. This resulted in compounds with low nanomolar activity. (C) 2009 Elsevier Ltd. All rights reserved.

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关键词

Bradykinin B-1,Antagonist,Oral bioavailability,Pharmacokinetic profile

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