Lead optimization of 5,6-diarylpyridines as CB1 receptor inverse agonists.

Christina B. Madsen-Duggan,John S. Debenham,Thomas F. Walsh,Richard B. Toupence,Song X. Huang,Junying Wang,Xinchun Tong,Julie Lao,Tung M. Fong,Marie Therese Schaeffer,Jing Chen Xiao,Cathy R.-R.C. Huang,Chun-Pyn Shen,D. Sloan Stribling,Lauren P. Shearman,Alison M. Strack,D. Euan MacIntyre,Lex H.T. Van der Ploeg,Mark T. Goulet

Lead optimization of 5,6-diarylpyridines as CB1 receptor inverse agonists.

2007

Christina B. Madsen-Duggan
John S. Debenham
Thomas F. Walsh
Richard B. Toupence
Song X. Huang
Junying Wang
Xinchun Tong
Julie Lao
Tung M. Fong
Marie Therese Schaeffer
Jing Chen Xiao
Cathy R.-R.C. Huang
Chun-Pyn Shen
D. Sloan Stribling
Lauren P. Shearman
Alison M. Strack
D. Euan MacIntyre
Lex H.T. Van der Ploeg
Mark T. Goulet

Optimization of the biological activity for 5,6-diarylpyridines as CB1 receptor inverse agonists is described. Food intake and pharmacokinetic evaluation of 3f and 15c indicate that these compounds are effective orally active modulators of CB1.

Keywords:

Oral administration
Inverse agonist
Biochemistry
In vivo
Cannabinoid
Organic chemistry
Structure–activity relationship
Biological activity
Pharmacokinetics
Cannabinoid receptor
Chemistry

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