2-Aryl-3,6-dialkyl-5-dialkylaminopyrimidin-4-ones as novel crf-1 receptor antagonists

Kevin J Hodgetts; Taeyoung Yoon; Jianhua Huang; Michael Gulianello; Andrzej Kieltyka; Renee Primus; Robbin Brodbeck; Stéphane De Lombaert; Darío Doller

doi:10.1016/s0960-894x(03)00483-9

2-Aryl-3,6-dialkyl-5-dialkylaminopyrimidin-4-ones as novel crf-1 receptor antagonists

Bioorg Med Chem Lett. 2003 Aug 4;13(15):2497-500. doi: 10.1016/s0960-894x(03)00483-9.

Authors

Kevin J Hodgetts¹, Taeyoung Yoon, Jianhua Huang, Michael Gulianello, Andrzej Kieltyka, Renee Primus, Robbin Brodbeck, Stéphane De Lombaert, Darío Doller

Affiliation

¹ Neurogen Corporation, 35NE Industrial Road, Branford, CT 06405, USA.

PMID: 12852951
DOI: 10.1016/s0960-894x(03)00483-9

Abstract

The discovery, synthesis and structure-activity studies of a novel series of 2-arylpyrimidin-4-ones as CRF-1 receptor antagonists is described. These compounds are structurally simple and display appropriate physical properties for CNS agents

MeSH terms

Chemical Phenomena
Chemistry, Physical
Drug Design
Humans
In Vitro Techniques
Indicators and Reagents
Microsomes / drug effects
Pyrimidines / chemical synthesis*
Pyrimidines / pharmacology*
Receptors, Corticotropin-Releasing Hormone / antagonists & inhibitors*
Structure-Activity Relationship

Substances

Indicators and Reagents
Pyrimidines
Receptors, Corticotropin-Releasing Hormone
CRF receptor type 1