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Discovery of potent and selective small molecule NPY Y5 receptor antagonists.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2002 Jul 08; Vol. 12 (13), pp. 1767-9. - Publication Year :
- 2002
-
Abstract
- The discovery of a new class of sulfonamide NPY Y5 receptor antagonists is described. Optimization of this series led to the identification of compounds with high affinity for the hY5 subtype and excellent selectivity over the other NPY receptor subtypes. The SAR for this series was examined and a model for understanding the ligand-receptor interactions was developed.
- Subjects :
- Animals
COS Cells
Histidine chemistry
Humans
Membrane Proteins chemistry
Membrane Proteins metabolism
Models, Molecular
Mutagenesis, Site-Directed
Protein Structure, Secondary
Radioligand Assay
Receptors, Neuropeptide Y metabolism
Stereoisomerism
Structure-Activity Relationship
Sulfonamides metabolism
Receptors, Neuropeptide Y antagonists & inhibitors
Receptors, Neuropeptide Y chemistry
Sulfonamides chemistry
Sulfonamides pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 12
- Issue :
- 13
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 12067557
- Full Text :
- https://doi.org/10.1016/s0960-894x(02)00287-1