Discovery of a New Class of Potent, Selective, and Orally Bioavailable CRTH2 (DP2) Receptor Antagonists for the Treatment of Allergic Inflammatory Diseases

A novel chemical class of potent chemoattractant receptor-homologous expressed on Th2 lymphocytes (CRTH2 or DP2) antagonists is reported. An initial and moderately potent spiro-indolinone compound (5) was found during a high-throughput screening campaign. Structure−activity relationship (SAR) invest...

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Veröffentlicht in:	Journal of medicinal chemistry 2008-04, Vol.51 (7), p.2227-2243
Hauptverfasser:	Crosignani, Stefano, Page, Patrick, Missotten, Marc, Colovray, Véronique, Cleva, Christophe, Arrighi, Jean-François, Atherall, John, Macritchie, Jackie, Martin, Thierry, Humbert, Yves, Gaudet, Marilène, Pupowicz, Doris, Maio, Maurizio, Pittet, Pierre-André, Golzio, Lucia, Giachetti, Claudio, Rocha, Cynthia, Bernardinelli, Gérald, Filinchuk, Yaroslav, Scheer, Alexander, Schwarz, Matthias K, Chollet, André
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Binding Sites Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Caco-2 Cells Cell Membrane Permeability - drug effects Crystallography, X-Ray Cytochrome P-450 Enzyme Inhibitors Dogs Drug Design Histamine and antagonists. Allergy Humans Hypersensitivity - drug therapy Indoles - chemistry Indoles - classification Indoles - pharmacology Inflammation - drug therapy Male Medical sciences Microsomes - drug effects Microsomes - metabolism Models, Molecular Molecular Structure Pharmacology. Drug treatments Rats Rats, Sprague-Dawley Receptors, Immunologic - antagonists & inhibitors Receptors, Prostaglandin - antagonists & inhibitors Spiro Compounds - chemistry Spiro Compounds - classification Spiro Compounds - pharmacology Stereoisomerism Structure-Activity Relationship
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