Preparation and Optimization of a Series of 3-Carboxamido-5-phenacylaminopyrazole Bradykinin B1 Receptor Antagonists

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...

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Veröffentlicht in:	Journal of medicinal chemistry 2007-10, Vol.50 (21), p.5161-5167
Hauptverfasser:	Dressen, Darren, Garofalo, Albert W, Hawkinson, Jon, Hom, Dennis, Jagodzinski, Jacek, Marugg, Jennifer L, Neitzel, Martin L, Pleiss, Michael A, Szoke, Balazs, Tung, Jay S, Wone, David W. G, Wu, Jing, Zhang, Heather
Format:	Artikel
Sprache:	eng
Schlagworte:	Benzamides - chemical synthesis Benzamides - chemistry Benzamides - pharmacology Biological and medical sciences Bradykinin B1 Receptor Antagonists Crystallography, X-Ray Fibroblasts - metabolism Humans In Vitro Techniques Lung - cytology Medical sciences Molecular Structure Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Pyrazoles - chemical synthesis Pyrazoles - chemistry Pyrazoles - pharmacology Radioligand Assay Structure-Activity Relationship
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