Purin-8-ones as corticotropin-releasing hormone (CRH-R1) receptor antagonists

JP Beck, AG Arvanitis, MA Curry, JT Rescinito…

Index: Beck, James P.; Arvanitis, Argyrios G.; Curry, Matt A.; Rescinito, Joseph T.; Fitzgerald, Larry W.; Gilligan, Paul J.; Zaczek, Robert; Trainor, George L. Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 7 p. 967 - 972

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Citation Number: 7

Abstract

A series of purin-8-ones was prepared and discovered to have excellent binding affintity 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.