Bioorganic and Medicinal Chemistry Letters 2011-Apr

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

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Phillip M Cowley

James Baker

Kirsteen I Buchanan

Ian Carlyle

John K Clark

Thomas R Clarkson

Maureen Deehan

Darren Edwards

Yasuko Kiyoi

Iain Martin

ARTICLE: 21334892

DOI: 10.1016/j.bmcl.2011.02.019

BioSeek: 21334892

Keywords

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.

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

Keywords

cannabinoid

indole

cannabis

Abstract

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