Synthesis and structure-activity relationships of a series of (1H-pyrazol-4-yl)acetamide antagonists of the P2X7 receptor

Chambers, Laura J, Stevens, Alexander J, Moses, Andrew P, Michel, Anton D, Walter, Daryl S, Davies, David J, Livermore, David G, Fonfria, Elena, Demont, Emmanuel H, Vimal, Mythily, Theobald, Pam J, Beswick, Paul J, Gleave, Robert J, Roman, Shilina A and Senger, Stefan (2010) Synthesis and structure-activity relationships of a series of (1H-pyrazol-4-yl)acetamide antagonists of the P2X7 receptor. Bioorganic & Medicinal Chemistry Letters, 20 (10). pp. 3161-4. ISSN 0960-894X

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Abstract

High-throughput screening identified compound 1 as a potent P2X(7) receptor antagonist suitable for lead optimisation. Structure-activity relationships (SAR) of a series of (1H-pyrazol-4-yl)acetamides were investigated and compound 32 was identified as a potent P2X(7) antagonist with enhanced potency and favourable physicochemical and pharmacokinetic properties.

Item Type: Article
Additional Information: Copyright 2010 Elsevier Ltd. All rights reserved.
Uncontrolled Keywords: acetamides,administration, oral,animals,anti-infective agents,high-throughput screening assays,humans,injections, intravenous,purinergic p2 receptor antagonists,pyrazoles,rats,receptors, purinergic p2,receptors, purinergic p2x7,structure-activity relationship
Faculty \ School: Faculty of Science > School of Biological Sciences
Depositing User: Pure Connector
Date Deposited: 06 Jan 2014 14:16
Last Modified: 25 Jul 2018 09:17
URI: https://ueaeprints.uea.ac.uk/id/eprint/46681
DOI: 10.1016/j.bmcl.2010.03.096

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