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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 Yaqoob
The 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 Chemistry

ISSN

0022-2623

Publisher

American Chemical Society

Issue

19

Volume

47

Page range

4642-4644

Department affiliated with

  • Chemistry Publications

Full text available

  • No

Peer reviewed?

  • Yes

Legacy Posted Date

2015-06-01

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