title: Application of a novel design paradigm to generate general nonpeptide combinatorial scaffolds mimicking beta turns: synthesis of ligands for somatostatin receptors.
abstract: Nonpeptide compounds that mimic bioactive peptides are desirable for a number of clinical indications. We report a new practical method for the design of scaffolds exhibiting drug-like properties that are suitable for the display of peptide pharmacophores. The synthesis of various synthons of 7'-hydroxy-2',3'-dihydro-1'H,2H,5H-spiro[imidazolidine-4,4'-quinoline]-2,5-dione (1) and methods for the introduction of several mimics of amino acid side-chains are described. This method is exemplified by derivatives that show agonist activity for the somatostatin type 2 receptor.
authors: ChemBridge Research Labs., LLC, 16981 Via Tazon, San Diego, CA 92127, USA.
authors: Dona
authors: D
authors: Chianelli
authors: Yong-Chul
authors: YC
authors: Kim
authors: Dmitriy
authors: D
authors: Lvovskiy
authors: Thomas R
authors: TR
authors: Webb
mesh_terms: D020650:Combinatorial Chemistry Techniques; D006827:Hydantoins / Q000737:chemistry; D009682:Magnetic Resonance Spectroscopy; D017481:Receptors, Somatostatin / Q000378:metabolism*; D021241:Spectrometry, Mass, Electrospray Ionization; D013141:Spiro Compounds / Q000737:chemistry
chemical_list: C488095:7'-hydroxy-2',3'-dihydro-1'H,2H,5H-spiro(imidazolidine-4,4'-quinoline)-2,5-dione; D006827:Hydantoins; D017481:Receptors, Somatostatin; D013141:Spiro Compounds; C093733:somatostatin receptor 2