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

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Cowley, Phillip M and Baker, James and Buchanan, Kirsteen I and Carlyle, Ian and Clark, John K and Clarkson, Thomas R and Deehan, Maureen and Edwards, Darren and Kiyoi, Yasuko and Martin, Iain and Osbourn, Dawn and Walker, Glenn and Ward, Nick and Wishart, Grant (2011) Pharmacokinetic optimisation of novel indole-2-carboxamide cannabinoid CB1 antagonists. Bioorganic and Medicinal Chemistry Letters, 21 (7). pp. 2034-2039. ISSN 0960-894X (https://doi.org/10.1016/j.bmcl.2011.02.019)

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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.

ORCID iDs

Cowley, Phillip M, Baker, James, Buchanan, Kirsteen I, Carlyle, Ian, Clark, John K, Clarkson, Thomas R, Deehan, Maureen, Edwards, Darren ORCID logoORCID: https://orcid.org/0000-0001-9544-8569, Kiyoi, Yasuko, Martin, Iain, Osbourn, Dawn, Walker, Glenn, Ward, Nick and Wishart, Grant;
CORE (COnnecting REpositories)