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

Research output: Contribution to journalArticle

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.

LanguageEnglish
Pages2034-2039
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume21
Issue number7
DOIs
Publication statusPublished - 1 Apr 2011

Fingerprint

Cannabinoid Receptor Antagonists
Pharmacokinetics
Cannabinoids
Biological Availability
indole
N-dodecyl-L-lysine amide

Keywords

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

Cite this

Cowley, P. M., Baker, J., Buchanan, K. I., Carlyle, I., Clark, J. K., Clarkson, T. R., ... 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
Cowley, Phillip M ; Baker, James ; Buchanan, Kirsteen I ; Carlyle, Ian ; Clark, John K ; Clarkson, Thomas R ; Deehan, Maureen ; Edwards, Darren ; Kiyoi, Yasuko ; Martin, Iain ; Osbourn, Dawn ; Walker, Glenn ; Ward, Nick ; Wishart, Grant. / Pharmacokinetic optimisation of novel indole-2-carboxamide cannabinoid CB1 antagonists. In: Bioorganic and Medicinal Chemistry Letters. 2011 ; Vol. 21, No. 7. pp. 2034-2039.
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Cowley, PM, Baker, J, Buchanan, KI, Carlyle, I, Clark, JK, Clarkson, TR, 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, vol. 21, no. 7, pp. 2034-2039. https://doi.org/10.1016/j.bmcl.2011.02.019

Pharmacokinetic optimisation of novel indole-2-carboxamide cannabinoid CB1 antagonists. / Cowley, Phillip M; Baker, James; Buchanan, Kirsteen I; Carlyle, Ian; Clark, John K; Clarkson, Thomas R; Deehan, Maureen; Edwards, Darren; Kiyoi, Yasuko; Martin, Iain; Osbourn, Dawn; Walker, Glenn; Ward, Nick; Wishart, Grant.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 21, No. 7, 01.04.2011, p. 2034-2039.

Research output: Contribution to journalArticle

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T1 - Pharmacokinetic optimisation of novel indole-2-carboxamide cannabinoid CB1 antagonists

AU - Cowley, Phillip M

AU - Baker, James

AU - Buchanan, Kirsteen I

AU - Carlyle, Ian

AU - Clark, John K

AU - Clarkson, Thomas R

AU - Deehan, Maureen

AU - Edwards, Darren

AU - Kiyoi, Yasuko

AU - Martin, Iain

AU - Osbourn, Dawn

AU - Walker, Glenn

AU - Ward, Nick

AU - Wishart, Grant

PY - 2011/4/1

Y1 - 2011/4/1

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KW - administration, oral

KW - biological availability

KW - humans

KW - indoles

KW - receptor, Cannabinoid, CB1

KW - structure-activity relationships

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U2 - 10.1016/j.bmcl.2011.02.019

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