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Issue 1, 2010
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Design, synthesis, and structure–activity relationships of indole-3-carboxamides as novel water soluble cannabinoid CB1 receptor agonists

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Abstract

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.

Graphical abstract: Design, synthesis, and structure–activity relationships of indole-3-carboxamides as novel water soluble cannabinoid CB1 receptor agonists

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Publication details

The article was received on 03 Mar 2010, accepted on 01 Apr 2010 and first published on 28 Apr 2010


Article type: Concise Article
DOI: 10.1039/C0MD00022A
Citation: Med. Chem. Commun., 2010,1, 54-60
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    Design, synthesis, and structure–activity relationships of indole-3-carboxamides as novel water soluble cannabinoid CB1 receptor agonists

    J. M. Adam, J. Cairns, W. Caulfield, P. Cowley, I. Cumming, M. Easson, D. Edwards, M. Ferguson, R. Goodwin, F. Jeremiah, T. Kiyoi, A. Mistry, E. Moir, R. Morphy, J. Tierney, M. York, J. Baker, J. E. Cottney, A. K. Houghton, P. J. Westwood and G. Walker, Med. Chem. Commun., 2010, 1, 54
    DOI: 10.1039/C0MD00022A

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