Several tetrahydroimidazopyrimidines were prepared using silver assisted cyclization as the key step. The binding affinities of compounds thus prepared were evaluated in vitro toward hCRF 1 R. Initial lead compound 16 ( K i = 32 nM) demonstrated modest putative anxiolytic effects in the mouse canopy test. Further optimization using parallel synthesis provided compounds with K i ’s <50 nM.
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Design, synthesis and evaluation of constrained tetrahydroimidazopyrimidine derivatives as antagonists of corticotropin-releasing factor type 1 receptor (CRF 1 R)
Vrudhula, Vivekananda M.; Dasgupta, Bireshwar; Pin, Sokhom S.; Burris, Kevin D.; Balanda, Lynn A.; Fung, Lawrence K.; Fiedler, Tracey; Browman, Kaitlin E.; Taber, Matthew T.; Zhang, Jie; Macor, John E.; Dubowchik, Gene M.
Follow Bioorganic & Medicinal Chemistry Letters
, Volume 20 (6)
Elsevier – Mar 15, 2010
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