Synthesis and evaluation of carbamate and aryl ether substituted pyrazinones as corticotropin releasing factor-1 (CRF₁) receptor antagonists.

Abstract

A series of pyrazinone-based compounds incorporating either carbamate or aryl ether groups was synthesized and evaluated as corticotropin-releasing factor-1 (CRF1) receptor antagonists. Structure-activity relationship studies led to the identification of highly potent CRF1 receptor antagonists 14a (IC50=0.74 nM) and 14b (IC50=1.9 nM). The synthesis, structure-activity relationships and in vitro metabolic stability properties of compounds in this series will be described.

DOI: 10.1016/j.bmcl.2016.03.067

Cite this paper

@article{Ahuja2016SynthesisAE, title={Synthesis and evaluation of carbamate and aryl ether substituted pyrazinones as corticotropin releasing factor-1 (CRF₁) receptor antagonists.}, author={Vijay Ahuja and Richard A Hartz and Thaddeus F. Molski and Gail K Mattson and Kimberley A. Lentz and James E Grace and Nicholas Lodge and Joanne J Bronson and John E. Macor}, journal={Bioorganic & medicinal chemistry letters}, year={2016}, volume={26 9}, pages={2184-7} }