Purin-8-ones as corticotropin-releasing hormone (CRH-R1) receptor antagonists |
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| Authors: | Beck J P Arvanitis A G Curry M A Rescinito J T Fitzgerald L W Gilligan P J Zaczek R Trainor G L |
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| Affiliation: | DuPont Pharmaceuticals Company, Chemical and Physical Sciences, Wilmington, DE 19880-0500, USA. |
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| Abstract: | 
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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