Bioorganic and Medicinal Chemistry Letters p. 967 - 972 (1999)
Update date:2022-08-03
Topics:
Beck, James P.
Arvanitis, Argyrios G.
Curry, Matt A.
Rescinito, Joseph T.
Fitzgerald, Larry W.
Gilligan, Paul J.
Zaczek, Robert
Trainor, George L.
A series of purin-8-ones was prepared and discovered to have excellent binding affinity to the CRH-R1 receptor. Structure-activity studies focused on amine side-chain optimization, urea substitution and pyridyl isostere incorporation. Thus, the highly potent purin-8-ones show promise as a new class of potential anxiolytics and/or antidepressants.
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