Potent and orally bioavailable non-peptide antagonists at the human bradykinin B1 receptor based on a 2-Alkylamino-5-sulfamoylbenzamide core

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 and Yaqoob, Mohammed (2004) Potent and orally bioavailable non-peptide antagonists at the human bradykinin B1 receptor based on a 2-Alkylamino-5-sulfamoylbenzamide core. Journal of Medicinal Chemistry, 47 (19). pp. 4642-4644. ISSN 0022-2623 (Submitted)

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Abstract

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.

Item Type: Article
Schools and Departments: School of Life Sciences > Chemistry
Subjects: Q Science > QD Chemistry
Depositing User: Tom Gittoes
Date Deposited: 01 Jun 2015 15:06
Last Modified: 01 Jun 2015 15:06
URI: http://sro.sussex.ac.uk/id/eprint/54217
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