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Bioorg Med Chem Lett. 2011 Mar 15;21(6):1748-53. doi: 10.1016/j.bmcl.2011.01.082. Epub 2011 Jan 22.

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

Author information

1
Department of Chemistry, Merck Research Laboratories, MSD, Newhouse, Lanarkshire, UK.

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.

PMID:
21316962
DOI:
10.1016/j.bmcl.2011.01.082
[Indexed for MEDLINE]

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