Synthesis of benzoylpyrimidines as antagonists of the corticotropin-releasing factor-1 receptor

Thomas R Webb; Terry Moran; Charles Q Huang; James R McCarthy; Dimitri E Grigoriadis; Chen Chen

doi:10.1016/j.bmcl.2004.05.072

Synthesis of benzoylpyrimidines as antagonists of the corticotropin-releasing factor-1 receptor

Bioorg Med Chem Lett. 2004 Aug 2;14(15):3869-73. doi: 10.1016/j.bmcl.2004.05.072.

Authors

Thomas R Webb¹, Terry Moran, Charles Q Huang, James R McCarthy, Dimitri E Grigoriadis, Chen Chen

Affiliation

¹ Department of Medicinal Chemistry and Department of Pharmacology, Neurocrine Bioscience, Inc., 10555 Science Center Drive, San Diego, CA 92121, USA.

PMID: 15225687
DOI: 10.1016/j.bmcl.2004.05.072

Abstract

A series of benzoylpyrimidines derived from the anilinepyrimidine CRF(1) antagonists were synthesized. Several synthetic routes were developed to explore the SAR of this series of compounds. Compounds such as 8d (K(i) = 15 nM) exhibited high binding affinities at the human CRF(1) receptor.

Publication types

Research Support, U.S. Gov't, P.H.S.

MeSH terms

Benzoates / chemical synthesis*
Benzoates / chemistry
Benzoates / pharmacology*
Cloning, Molecular
Humans
Models, Molecular
Molecular Conformation
Molecular Structure
Pyrimidines / chemical synthesis*
Pyrimidines / chemistry
Pyrimidines / pharmacology*
Receptors, Corticotropin-Releasing Hormone / antagonists & inhibitors*
Structure-Activity Relationship
Thermodynamics

Substances

Benzoates
Pyrimidines
Receptors, Corticotropin-Releasing Hormone
CRF receptor type 1

Grants and funding

1R43 NS 334879/NS/NINDS NIH HHS/United States