3-Aryl pyrazolo[4,3-d]pyrimidine derivatives: Nonpeptide CRF-1 antagonists

Jun Yuan; Michael Gulianello; Stéphane De Lombaert; Robbin Brodbeck; Andrzej Kieltyka; Kevin J Hodgetts

doi:10.1016/s0960-894x(02)00358-x

3-Aryl pyrazolo[4,3-d]pyrimidine derivatives: Nonpeptide CRF-1 antagonists

Bioorg Med Chem Lett. 2002 Aug 19;12(16):2133-6. doi: 10.1016/s0960-894x(02)00358-x.

Authors

Jun Yuan¹, Michael Gulianello, Stéphane De Lombaert, Robbin Brodbeck, Andrzej Kieltyka, Kevin J Hodgetts

Affiliation

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

PMID: 12127521
DOI: 10.1016/s0960-894x(02)00358-x

Abstract

The synthesis of a series of 3-aryl pyrazolo[4,3-d]pyrimidines as potential corticotropin-releasing factor (CRF-1) antagonists is described. The effects of substitution on the aromatic ring, the amino group and the pyrazolo ring on CRF-1 receptor binding were investigated.

MeSH terms

Binding Sites
Drug Design*
Molecular Structure
Pyrimidines / chemical synthesis*
Pyrimidines / chemistry
Pyrimidines / pharmacology*
Receptors, Corticotropin-Releasing Hormone / antagonists & inhibitors*
Structure-Activity Relationship

Substances

Pyrimidines
Receptors, Corticotropin-Releasing Hormone
CRF receptor type 1