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Bioorg Med Chem Lett
; 19(6): 1702-6, 2009 Mar 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-19231185
RESUMEN
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 delta-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.