945757-15-3Relevant academic research and scientific papers
Discovery of pyrazine carboxamide CB1 antagonists: The introduction of a hydroxyl group improves the pharmaceutical properties and in vivo efficacy of the series
Ellsworth, Bruce A.,Wang, Ying,Zhu, Yeheng,Pendri, Annapurna,Gerritz, Samuel W.,Sun, Chongqing,Carlson, Kenneth E.,Kang, Liya,Baska, Rose A.,Yang, Yifan,Huang, Qi,Burford, Neil T.,Cullen, Mary Jane,Johnghar, Susan,Behnia, Kamelia,Pelleymounter, Mary Ann,Washburn, William N.,Ewing, William R.
, p. 3978 - 3982 (2008/02/07)
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.
