Bioorganic & Medicinal Chemistry Letters 2010-02-01

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

Index: Bioorg. Med. Chem. Lett. 20(3) , 1229-32, (2010)

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Abstract

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.Copyright (c) 2009 Elsevier Ltd. All rights reserved.