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Discovery of potent and orally bioavailable heterocycle-based cannabinoid CB1 receptor agonists

Kiyoi, Takao and Adam, Julia M and Clark, John K and Davies, Keneth and Easson, Anna-Marie and Edwards, Darren and Feilden, Helen and Fields, Ruth and Francis, Stuart and Jeremiah, Fiona and McArthur, Duncan and Morrison, Angus J and Prosser, Alan and Ratcliffe, Paul D and Schulz, Jurgen and Wishart, Grant and Baker, James and Campbell, Robert and Cottney, Jean E and Deehan, Maureen and Epemolu, Ola and Evans, Louise (2011) Discovery of potent and orally bioavailable heterocycle-based cannabinoid CB1 receptor agonists. Bioorganic and Medicinal Chemistry Letters, 21 (6). pp. 1748-1753. ISSN 0960-894X

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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.