Design, synthesis, and structure-activity relationships of indole-3-carboxamides as novel water soluble cannabinoid CB1 receptor agonistsElectronic supplementary information (ESI) available: Experimental data for compounds 1 to 35 and materials and methods for in vitro and in vivo assays. See DOI: 10.1039/c0md00022a

A novel CB1 receptor agonist lead series was identified using a high-throughput screening approach. The initial screen afforded a single confirmed hit with poor water solubility. Structural variations were explored with the aim of introducing water solubility and improving potency. This led to the d...

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Main Authors: Adam, Julia M, Cairns, Jim, Caulfield, Wilson, Cowley, Phillip, Cumming, Iain, Easson, Morag, Edwards, Darren, Ferguson, Morag, Goodwin, Richard, Jeremiah, Fiona, Kiyoi, Takao, Mistry, Ashvin, Moir, Elizabeth, Morphy, Richard, Tierney, Jason, York, Mark, Baker, James, Cottney, Jean E, Houghton, Andrea K, Westwood, Paul J, Walker, Glenn
Format: Article
Language:English
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Summary:A novel CB1 receptor agonist lead series was identified using a high-throughput screening approach. The initial screen afforded a single confirmed hit with poor water solubility. Structural variations were explored with the aim of introducing water solubility and improving potency. This led to the discovery of Org 28611, a potent, water soluble CB1 receptor agonist, which was selected for clinical evaluation as a potential intravenous analgesic agent. A novel CB1 receptor agonist clinical candidate was identified using high-throughput screening followed by optimization of potency and physico-chemical properties.
ISSN:2040-2503
2040-2511
DOI:10.1039/c0md00022a