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

J P Beck; A G Arvanitis; M A Curry; J T Rescinito; L W Fitzgerald; P J Gilligan; R Zaczek; G L Trainor

doi:10.1016/s0960-894x(99)00108-0

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

Bioorg Med Chem Lett. 1999 Apr 5;9(7):967-72. doi: 10.1016/s0960-894x(99)00108-0.

Authors

J P Beck¹, A G Arvanitis, M A Curry, J T Rescinito, L W Fitzgerald, P J Gilligan, R Zaczek, G L Trainor

Affiliation

¹ DuPont Pharmaceuticals Company, Chemical and Physical Sciences, Wilmington, DE 19880-0500, USA.

PMID: 10230622
DOI: 10.1016/s0960-894x(99)00108-0

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.

MeSH terms

Anti-Anxiety Agents / chemistry
Anti-Anxiety Agents / pharmacology
Antidepressive Agents / chemistry
Antidepressive Agents / pharmacology
Purinones / chemistry
Purinones / pharmacology*
Receptors, Corticotropin-Releasing Hormone / antagonists & inhibitors*
Structure-Activity Relationship

Substances

Anti-Anxiety Agents
Antidepressive Agents
Purinones
Receptors, Corticotropin-Releasing Hormone
CRF receptor type 1