Discovery of 5-Arylsulfonamido-3- (pyrrolidin-2-ylmethyl)-1H-indole Derivatives as Potent, Selective 5-HT6 Receptor Agonists and Antagonists

Autor: Cole, D. C., Lennox, W. J., Lombardi, S., Ellingboe, J. W., Bernotas, R. C., Tawa, G. J., Mazandarani, H., Smith, D. L., Zhang, G., Coupet, J., Schechter, L. E.
Zdroj: Journal of Medicinal Chemistry; January 2005, Vol. 48 Issue: 2 p353-356, 4p
Abstrakt: 5-Arylsulfonylamido-3-(pyrrolidin-2-ylmethyl)-1H-indoles have been identified as high-affinity 5-HT6 receptor ligands. Within this class, several of the (R)-enantiomers were potent agonists having EC50 values of 1 nM or less and functioning as full agonists while the (S)-enantiomers displayed moderate antagonist activity.
Databáze: Supplemental Index