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J Med Chem. 2007 Oct 18;50(21):5161-7. Epub 2007 Sep 19.

Preparation and optimization of a series of 3-carboxamido-5-phenacylaminopyrazole bradykinin B1 receptor antagonists.

Author information

1
Elan Pharmaceuticals, Inc., 800 Gateway Boulevard, South San Francisco, California 94080, USA. al.garofalo@elan.com

Abstract

The B1 receptor is an attractive target for the treatment of pain and inflammation. A series of 3-carboxamido-5-phenacylamino pyrazole B1 receptor antagonists are described that exhibit good potency against B1 and high selectivity over B2. Initially, N-unsubstituted pyrazoles were studied, but these compounds suffered from extensive glucuronidation in primates. This difficulty could be surmounted by the use of N-substituted pyrazoles. Optimization efforts culminated in compound 41, which has high receptor potency and metabolic stability.

PMID:
17880055
DOI:
10.1021/jm051292n
[Indexed for MEDLINE]

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