Abstract:
:A series of 5,6-diaryl-2-amino-pyrazines were prepared and found to have antagonist-like properties at the CB1 receptor. Subsequent SAR studies optimized both receptor potency and drug-like properties including solubility and Cytochrome-P450 inhibition potential. Optimized compounds were demonstrated to be inverse agonists and compared in vivo with rimonabant for their ability to inhibit food intake, to occupy central CB1 receptors and to influence hormonal markers associated with obesity.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Wustrow DJ,Maynard GD,Yuan J,Zhao H,Mao J,Guo Q,Kershaw M,Hammer J,Brodbeck RM,Near KE,Zhou D,Beers DS,Chenard BL,Krause JE,Hutchison AJdoi
10.1016/j.bmcl.2008.04.022subject
Has Abstractpub_date
2008-06-01 00:00:00pages
3376-81issue
11eissn
0960-894Xissn
1464-3405pii
S0960-894X(08)00412-5journal_volume
18pub_type
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