Potent Dihydroquinolinone Dopamine D2 Partial Agonist/Serotonin Reuptake Inhibitors for the Treatment of Schizophrenia

Authors

Yinfa Yan, Wyeth Research
Ping Zhou, Solvay Pharmaceuticals Research Laboratories
David Rotella, Montclair State UniversityFollow
Rolf Feenstra, Solvay S.A.Follow
Chris G. Kruse, Solvay S.A.
Jan Hendrik Reinders, Solvay S.A.
Martina van der Neut, Solvay S.A.Follow
Margaret Lai, Wyeth ResearchFollow
Jean Zhang, Wyeth ResearchFollow
Dianne M. Kowal, Wyeth Research
Tikva Carrick, Wyeth ResearchFollow
Karen L. Marquis, PfizerFollow
Mark H. Pausch, Wyeth ResearchFollow
Albert J. Robichaud, Sage Therapeutics, Inc.

Document Type

Article

Publication Date

5-1-2010

Journal / Book Title

Bioorganic & Medicinal Chemistry Letters

Abstract

A dihydroquinolinone moiety was found to be a potent serotonin reuptake inhibitor pharmacophore when combined with certain amines. This fragment was coupled with selected D2 ligands to prepare a series of dual acting compounds with attractive in vitro profiles as dopamine D2 partial agonists and serotonin reuptake inhibitors. Structure-activity studies revealed that the linker plays a key role in contributing to D2 affinity, function, and SRI activity.

DOI

10.1016/j.bmcl.2010.02.105

Montclair State University Digital Commons Citation

Yan, Yinfa; Zhou, Ping; Rotella, David; Feenstra, Rolf; Kruse, Chris G.; Reinders, Jan Hendrik; Neut, Martina van der; Lai, Margaret; Zhang, Jean; Kowal, Dianne M.; Carrick, Tikva; Marquis, Karen L.; Pausch, Mark H.; and Robichaud, Albert J., "Potent Dihydroquinolinone Dopamine D2 Partial Agonist/Serotonin Reuptake Inhibitors for the Treatment of Schizophrenia" (2010). Department of Chemistry and Biochemistry Faculty Scholarship and Creative Works. 23.
https://digitalcommons.montclair.edu/chem-biochem-facpubs/23