Pyrazolopyridazine alpha-2-delta-1 ligands for the treatment of neuropathic pain

Myatt, James W, Healy, Mark P, Bravi, Gianpaolo S, Billinton, Andrew, Johnson, Christopher N, Matthews, Kim L, Jandu, Karamjit S, Meng, Wenjing, Hersey, Anne, Livermore, David G, Douault, Clement B, Witherington, Jason, Bit, Rino A, Rowedder, James E, Brown, Jason D and Clayton, Nick M (2010) Pyrazolopyridazine alpha-2-delta-1 ligands for the treatment of neuropathic pain. Bioorganic & Medicinal Chemistry Letters, 20 (15). pp. 4683-8. ISSN 0960-894X

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Abstract

Optimization of the novel alpha-2-delta-1 ligand 4 provided compounds 37 and 38 which have improved DMPK profiles, good in vivo analgesic activity and in vitro selectivity over alpha-2-delta-2. An in-house P-gp prediction programme and the MetaSite software package were used to help solve the specific problems of high P-gp efflux and high in vivo clearance.

Item Type: Article
Additional Information: Copyright 2010 Elsevier Ltd. All rights reserved.
Uncontrolled Keywords: analgesics,animals,calcium channel blockers,calcium channels,ligands,neuralgia,p-glycoprotein,pyrazoles,pyridazines,pyridines,rats,structure-activity relationship
Faculty \ School: Faculty of Medicine and Health Sciences > Norwich Medical School
Depositing User: Pure Connector
Date Deposited: 20 Jan 2014 16:56
Last Modified: 23 Jan 2019 13:50
URI: https://ueaeprints.uea.ac.uk/id/eprint/46678
DOI: 10.1016/j.bmcl.2010.05.026

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