Pharmacokinetic optimisation of novel indole-2-carboxamide cannabinoid CB1 antagonists

Phillip M Cowley, James Baker, Kirsteen I Buchanan, Ian Carlyle, John K Clark, Thomas R Clarkson, Maureen Deehan, Darren Edwards, Yasuko Kiyoi, Iain Martin, Dawn Osbourn, Glenn Walker, Nick Ward, Grant Wishart

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3 Citations (Scopus)

Abstract

The pharmacokinetic based optimisation of a novel series of indole-2-carboxamide antagonists of the cannabinoid CB(1) receptor is disclosed. Compound 24 was found to be a highly potent and selective cannabinoid CB(1) antagonist with high predicted human oral bioavailability.

Original languageEnglish
Pages (from-to)2034-2039
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume21
Issue number7
DOIs
Publication statusPublished - 1 Apr 2011

Keywords

  • administration, oral
  • biological availability
  • humans
  • indoles
  • receptor, Cannabinoid, CB1
  • structure-activity relationships

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    Cowley, P. M., Baker, J., Buchanan, K. I., Carlyle, I., Clark, J. K., Clarkson, T. R., Deehan, M., Edwards, D., Kiyoi, Y., Martin, I., Osbourn, D., Walker, G., Ward, N., & Wishart, G. (2011). Pharmacokinetic optimisation of novel indole-2-carboxamide cannabinoid CB1 antagonists. Bioorganic and Medicinal Chemistry Letters, 21(7), 2034-2039. https://doi.org/10.1016/j.bmcl.2011.02.019