| Literature DB >> 21316962 |
Takao Kiyoi1, 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, James Baker, Robert Campbell, Jean E Cottney, Maureen Deehan, Ola Epemolu, Louise Evans.
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.Entities:
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Year: 2011 PMID： 21316962 DOI： 10.1016/j.bmcl.2011.01.082
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823