Identification of 3-sulfonylindazole derivatives as potent and selective 5-HT(6) antagonists.

Autor: Liu KG; Chemical Sciences, Wyeth Research, CN 8000, Princeton, NJ 08543, USA. liuk@lundbeck.com, Robichaud AJ, Greenfield AA, Lo JR, Grosanu C, Mattes JF, Cai Y, Zhang GM, Zhang JY, Kowal DM, Smith DL, Di L, Kerns EH, Schechter LE, Comery TA
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry [Bioorg Med Chem] 2011 Jan 01; Vol. 19 (1), pp. 650-62. Date of Electronic Publication: 2010 Oct 20.
DOI: 10.1016/j.bmc.2010.10.033
Abstrakt: As part of our efforts to develop agents for cognitive enhancement, we have been focused on the 5-HT(6) receptor in order to identify potent and selective ligands for this purpose. Herein we report the identification of a novel series of 3-sulfonylindazole derivatives with acyclic amino side chains as potent and selective 5-HT(6) antagonists. The synthesis and detailed SAR of this class of compounds are reported.
(Copyright © 2010 Elsevier Ltd. All rights reserved.)
Databáze: MEDLINE