Title of article
Discovery of pyrazine carboxamide CB1 antagonists: The introduction of a hydroxyl group improves the pharmaceutical properties and in vivo efficacy of the series
Author/Authors
Bruce A. Ellsworth، نويسنده , , Ying Wang، نويسنده , , Yeheng Zhu، نويسنده , , Annapurna Pendri، نويسنده , , Samuel W. Gerritz، نويسنده , , Chongqing Sun، نويسنده , , Kenneth E. Carlson، نويسنده , , Liya Kang، نويسنده , , Rose A. Baska، نويسنده , , Yifan Yang، نويسنده , , Qi Huang، نويسنده , , Neil T. Burford، نويسنده , , Mary Jane Cullen، نويسنده , , Susan Johnghar، نويسنده , , Kamelia Behnia، نويسنده , , Mary Ann Pelleymounter، نويسنده , , William N. Washburn، نويسنده , , William R. Ewing، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
5
From page
3978
To page
3982
Abstract
Structure–activity relationships for a series of pyrazine carboxamide CB1 antagonists are reported. Pharmaceutical properties of the series are improved via inclusion of hydroxyl-containing sidechains. This structural modification sufficiently improved ADME properties of an orally inactive series such that food intake reduction was achieved in rat feeding models. Compound 35 elicits a 46% reduction in food intake in ad libidum fed rats 4-h post-dose.
Keywords
CB1 , GPCR , Cannabinoid , obesity , pyrazine , ADME , hypophagia , Antagonist
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798351
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