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5-HT2C antagonists based on fused heterotricyclic templates: design, synthesis and biological evaluation.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Jan 15; Vol. 17 (2), pp. 424-7. Date of Electronic Publication: 2006 Oct 17. - Publication Year :
- 2007
-
Abstract
- Design, synthesis and properties of a new tricyclic series of selective 5-HT2C receptor antagonists are reported. Conformational analysis of a 2-phenyl-dihydropyrrolone scaffold suggested that ring fusion, locking coplanarity between the rings of this moiety, might be tolerated by the 5-HT2C receptor. An interesting effect of this is the change of the nature of the carbon-carbon double bond of the lactam ring from vinylic to aromatic. The changes were found to result in a favourable profile at both, receptor and in vivo level.
- Subjects :
- Alkylation
Animals
Biological Availability
Drug Design
Heterocyclic Compounds pharmacokinetics
Humans
Indicators and Reagents
Male
Models, Molecular
Molecular Conformation
Rats
Receptor, Serotonin, 5-HT2A drug effects
Receptor, Serotonin, 5-HT2B drug effects
Structure-Activity Relationship
Heterocyclic Compounds chemical synthesis
Heterocyclic Compounds pharmacology
Receptor, Serotonin, 5-HT2C drug effects
Serotonin Antagonists pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 17
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 17079142
- Full Text :
- https://doi.org/10.1016/j.bmcl.2006.10.034