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

doi:10.1016/j.bmcl.2011.02.019

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

Strathclyde Institute Of Pharmacy And Biomedical Sciences

Research output: Contribution to journal › Article › peer-review

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 language	English
Pages (from-to)	2034-2039
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	21
Issue number	7
DOIs	https://doi.org/10.1016/j.bmcl.2011.02.019
Publication status	Published - 1 Apr 2011

Keywords

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

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10.1016/j.bmcl.2011.02.019

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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

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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.",

keywords = "administration, oral, biological availability, humans, indoles, receptor, Cannabinoid, CB1, structure-activity relationships",

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

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doi = "10.1016/j.bmcl.2011.02.019",

language = "English",

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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

TY - JOUR

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

N2 - 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.

AB - 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.

KW - administration, oral

KW - biological availability

KW - humans

KW - indoles

KW - receptor, Cannabinoid, CB1

KW - structure-activity relationships

UR - http://www.journals.elsevier.com/bioorganic-and-medicinal-chemistry-letters

U2 - 10.1016/j.bmcl.2011.02.019

DO - 10.1016/j.bmcl.2011.02.019

M3 - Article

C2 - 21334892

SN - 0960-894X

VL - 21

SP - 2034

EP - 2039

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 7

ER -

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

Abstract

Keywords

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