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Potent and orally bioavailable non-peptide antagonists at the human bradykinin B1 receptor based on a 2-Alkylamino-5-sulfamoylbenzamide core
journal contribution
posted on 2023-06-08, 20:57 authored by Timothy J Ritchie, Edward K Dziadulewicz, Andrew J Culshaw, Werner Müller, Gillian M Burgess, Graham C Bloomfield, Gillian S Drake, Andrew R Dunstan, David Beattie, Glyn A Hughes, Pam Ganju, Peter McIntyre, Stuart J Bevan, Clare Davis, Mohammed YaqoobThe bradykinin B(1) 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 B(1) receptor antagonists based on a 2-alkylamino-5-sulfamoylbenzamide core. Optimized derivatives are selective, functional B(1) antagonists with low nanomolar affinity and exhibit oral bioavailability in animals.
History
Publication status
- Published
Journal
Journal of Medicinal ChemistryISSN
0022-2623Publisher
American Chemical SocietyExternal DOI
Issue
19Volume
47Page range
4642-4644Department affiliated with
- Chemistry Publications
Full text available
- No
Peer reviewed?
- Yes
Legacy Posted Date
2015-06-01Usage metrics
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