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

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

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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.