| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1371435 | Bioorganic & Medicinal Chemistry Letters | 2011 | 6 Pages |
Abstract
Novel 3-(1H-indol-3-yl)-1,2,4-oxadiazoles and -thiadiazoles were synthesized and found to be potent CB1 cannabinoid receptor agonists. The oral bioavailability of these compounds could be dramatically improved by optimization studies of the side chains attached to the indole and oxadiazole cores, leading to identification of a CB1 receptor agonist with good oral activity in a range of preclinical models of antinociception and antihyperalgesia.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Takao Kiyoi, Julia M. Adam, John K. Clark, Keneth Davies, Anna-Marie Easson, Darren Edwards, Helen Feilden, Ruth Fields, Stuart Francis, Fiona Jeremiah, Duncan McArthur, Angus J. Morrison, Alan Prosser, Paul D. Ratcliffe, Jurgen Schulz, Grant Wishart,