Pyridopyrimidine based cannabinoid-1 receptor inverse agonists: Synthesis and biological evaluation.
The synthesis, SAR and binding affinities are described for cannabinoid-1 receptor (CB1R) specific inverse agonists based on pyridopyrimidine and heterotricyclic scaffolds. Food intake and pharmacokinetic evaluation of several of these compounds indicate that they are effective orally active modulators of CB1R.
Debenham
John S
JS
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA.
Madsen-Duggan
Christina B
CB
Wang
Junying
J
Tong
Xinchun
X
Lao
Julie
J
Fong
Tung M
TM
Schaeffer
Marie-Therese
MT
Xiao
Jing Chen
JC
Huang
Cathy C R-R
CC
Shen
Chun-Pyn
CP
Sloan Stribling
D
D
Shearman
Lauren P
LP
Strack
Alison M
AM
Euan Macintyre
D
D
Hale
Jeffrey J
JJ
Walsh
Thomas F
TF