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Updated: Jun 12, 2026

Preparation and In Vivo Use of an Activity-based Probe for N-acylethanolamine Acid Amidase
Published on: November 23, 2016
Aryl sulfonamides containing tetralin allylic amines as potent and selective bradykinin B1 receptor antagonists
Qingyian Liu1, Wenyuan Qian, Aiwen Li
1Chemistry Research and Discovery, Amgen Inc., Thousand Oaks, CA 91320, USA. qingyian@amgen.com
Abstract:
The bradykinin B1 receptor has been shown to mediate pain response and is rapidly induced upon injury. Blocking this receptor may provide a promising treatment for inflammation and pain. We previously reported tetralin benzyl amines as potent B1 antagonists. Here we describe the synthesis and SAR of B1 receptor antagonists with homobenzylic amines. The SAR of different linkers led to the discovery of tetralin allylic amines as potent and selective B1 receptor antagonists (hB1 IC(50)=1.3 nM for compound 16). Some of these compounds showed modest oral bioavailability in rats.
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