1. 3,4-Dihydro-2H-benzo[1,4]oxazine derivatives as 5-HT6 receptor antagonists.
- Author
-
Zhao SH, Berger J, Clark RD, Sethofer SG, Krauss NE, Brothers JM, Martin RS, Misner DL, Schwab D, and Alexandrova L
- Subjects
- Animals, Models, Chemical, Oxazines chemical synthesis, Rats, Receptors, Serotonin metabolism, Serotonin Antagonists chemical synthesis, Structure-Activity Relationship, Oxazines pharmacology, Receptors, Serotonin drug effects, Serotonin Antagonists pharmacology
- Abstract
A series of novel 3,4-dihydro-2H-benzo[1,4]oxazine derivatives has been designed and synthesized as 5-HT(6) receptor antagonists. Many of the compounds displayed subnanomolar affinities for the 5-HT(6) receptor and good brain penetration in rats. The relationship of structure and lipophilicity to hERG inhibition of this series of compounds is discussed.
- Published
- 2007
- Full Text
- View/download PDF