H. Hunt, J. Belanoff, E. Golding
Dec 15, 2015
Citations
2
Influential Citations
20
Citations
Journal
Bioorganic & medicinal chemistry letters
Abstract
We report the further optimization of our series 1H-pyrazolo[3,4-g]hexahydro-isoquinoline sulfonamides as GR antagonists. By incorporating a heteroaryl ketone group at the ring junction, we have obtained compounds with excellent functional GR antagonism. Optimization of the sulfonamide substituent has provided compounds with a very desirable overall profile, including minimal hERG activity, good bioavailability and in vivo efficacy.