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Synthesis and evaluation of spirobenzazepines as potent vasopressin receptor antagonists
- Source :
- Bioorganic & Medicinal Chemistry Letters. 14:2987-2989
- Publication Year :
- 2004
- Publisher :
- Elsevier BV, 2004.
-
Abstract
- A novel series of spirobenzazepines was synthesized and evaluated for V1a and V2 receptor antagonist activity. Compounds 8b, 8i, and 8k have shown selective V1a receptor antagonist activity. Compounds 8p and 8q were shown to be dual V1a/V2 receptor antagonists.
- Subjects :
- Stereochemistry
Vasopressin Receptor Antagonists
Clinical Biochemistry
Pharmaceutical Science
Pharmacology
Ligands
Biochemistry
Chemical synthesis
Cell Line
Inhibitory Concentration 50
Structure-Activity Relationship
Arginine vasopressin receptor 2
Drug Discovery
Cyclic AMP
Humans
Spiro Compounds
Molecular Biology
Chemistry
Organic Chemistry
Antagonist
Biological activity
General Medicine
Benzazepines
V1a vasopressin receptor
In vitro
Competitive antagonist
Molecular Medicine
Antidiuretic Hormone Receptor Antagonists
Receptor antagonist activity
Protein Binding
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 14
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....cb9877d3be8611d36b02f45cb0367cb9
- Full Text :
- https://doi.org/10.1016/j.bmcl.2004.02.103