| Autor: |
Owen DR; Pfizer Global Research and Development, Sandwich Laboratories, Ramsgate Road, Sandwich, CT13 9NJ, UK., Rodriguez-Lens M, Corless MD, Gaulier SM, Horne VA, Kinloch RA, Maw GN, Pearce DW, Rees H, Ringer TJ, Ryckmans T, Stammen BL |
| Jazyk: |
angličtina |
| Zdroj: |
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2009 Mar 15; Vol. 19 (6), pp. 1702-6. Date of Electronic Publication: 2009 Feb 05. |
| DOI: |
10.1016/j.bmcl.2009.01.106 |
| Abstrakt: |
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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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