Details

Autor(en) / Beteiligte

• Ritchie, Timothy J
• Dziadulewicz, Edward K
• Culshaw, Andrew J
• Müller, Werner
• Burgess, Gillian M
• Bloomfield, Graham C
• Drake, Gillian S
• Dunstan, Andrew R
• Beattie, David
• Hughes, Glyn A
• Ganju, Pam
• McIntyre, Peter
• Bevan, Stuart J
• Davis, Clare
• Yaqoob, Mohammed

Titel

Potent and Orally Bioavailable Non-Peptide Antagonists at the Human Bradykinin B1 Receptor Based on a 2-Alkylamino-5-sulfamoylbenzamide Core

Ist Teil von

• Journal of medicinal chemistry, 2004-09, Vol.47 (19), p.4642-4644

Ort / Verlag

Washington, DC: American Chemical Society

Erscheinungsjahr

2004

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• The bradykinin B1 receptor is rapidly induced after inflammation or tissue trauma and appears to play an important role in the maintenance of hyperalgesia in inflammatory conditions. Here, we describe the optimization process to identify novel, potent non-peptide human B1 receptor antagonists based on a 2-alkylamino-5-sulfamoylbenzamide core. Optimized derivatives are selective, functional B1 antagonists with low nanomolar affinity and exhibit oral bioavailability in animals.