2,4-Diaminopyridine δ-opioid receptor agonists and their associated hERG pharmacology

Owen, Dafydd R, Rodriguez-Lens, Margarita, Corless, Martin D, Gaulier, Steven M, Horne, Valerie A, Kinloch, Ross A, Maw, Graham N, Pearce, David W, Rees, Huw, Ringer, Tracy J, Ryckmans, Thomas and Stammen, Blanda L C (2009) 2,4-Diaminopyridine δ-opioid receptor agonists and their associated hERG pharmacology. Bioorganic and Medicinal Chemistry Letters, 19 (6). pp. 1702-1706. ISSN 0960-894X

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Abstract

A number of libraries were produced to explore the potential of 2,4-diaminopyridine lead 1. The resulting diaminopyridines proved to be potent and selective δ-opioid receptor agonists. Several rounds of lead optimisation using library chemistry identified compound 17 which went on to show efficacy in an electromyography model of neuropathic pain. The structure–activity relationship of the series against the hERG ion channel proved to be a key selectivity hurdle for the series.

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 10:38
Last Modified: 01 Jun 2015 10:38
URI: http://sro.sussex.ac.uk/id/eprint/54178
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