High-throughput synthesis optimization of sulfonamide NPY Y5 antagonists
| Autor: | John T. Finn, David Pelham, Mary W. Walker, Charles Gluchowski |
|---|---|
| Rok vydání: | 2002 |
| Předmět: |
Y5 Receptor
medicine.drug_class Stereochemistry Clinical Biochemistry Pharmaceutical Science Carboxamide Biochemistry Chemical synthesis Radioligand Assay Structure-Activity Relationship Drug Discovery medicine Animals Humans Urea Amines Molecular Biology chemistry.chemical_classification Sulfonamides Cell Membrane Organic Chemistry Neuropeptide Y receptor Combinatorial chemistry Receptors Neuropeptide Y Sulfonamide chemistry Drug Design COS Cells Molecular Medicine Protein Binding |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 12:1771-1774 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/s0960-894x(02)00288-3 |
| Popis: | A series of sulfonamide neuropeptide Y Y5 antagonists was optimized by preparation of sets of analogues using high-throughput synthesis and purification techniques. Testing of these compounds for their ability to bind to the human NPY Y5 receptor revealed separate SAR trends for sulfonamide amides versus sulfonamide ureas versus sulfonamide amines. By understanding these SAR trends, potent compounds were identified in all three series. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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