Potential CRF1R PET imaging agents: 1-fluoroalkylsubstituted 5-halo-3-(arylamino)pyrazin-2(1H)-ones

Derek J Denhart; Dmitry Zuev; Jonathan L Ditta; Richard A Hartz; Vijay T Ahuja; Ronald J Mattson; Hong Huang; Gail K Mattson; Larisa Zueva; Julia M Nielsen; Edward S Kozlowski; Nicholas J Lodge; Joanne J Bronson; John E Macor

doi:10.1016/j.bmcl.2013.02.009

Potential CRF1R PET imaging agents: 1-fluoroalkylsubstituted 5-halo-3-(arylamino)pyrazin-2(1H)-ones

Bioorg Med Chem Lett. 2013 Apr 1;23(7):2052-5. doi: 10.1016/j.bmcl.2013.02.009. Epub 2013 Feb 13.

Authors

Derek J Denhart¹, Dmitry Zuev, Jonathan L Ditta, Richard A Hartz, Vijay T Ahuja, Ronald J Mattson, Hong Huang, Gail K Mattson, Larisa Zueva, Julia M Nielsen, Edward S Kozlowski, Nicholas J Lodge, Joanne J Bronson, John E Macor

Affiliation

¹ Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA. derek.denhart@bms.com

PMID: 23465610
DOI: 10.1016/j.bmcl.2013.02.009

Abstract

A series of pyrazinones were prepared and evaluated as potential CRF(1)R PET imaging agents. Optimization of their CRF(1)R binding potencies and octanol-phosphate buffer phase distribution coefficients are discussed herein.

MeSH terms

Animals
Brain
Humans
Molecular Structure
Positron-Emission Tomography*
Pyrazines / chemistry
Pyrazines / pharmacology*
Rats
Receptors, Corticotropin-Releasing Hormone / antagonists & inhibitors*
Receptors, Corticotropin-Releasing Hormone / chemistry

Substances

Pyrazines
Receptors, Corticotropin-Releasing Hormone
CRF receptor type 1