Potent antagonists of the CCR2b receptor. Part 3: SAR of the ( R)-3-aminopyrrolidine series

SAR studies of a 3-amino pyrrolidine series led to the identification of potent CCR2b antagonists with low nanomolar activity in binding and functional assays as exemplified by compound 71. SAR studies were conducted around lead compound 1 using high-throughput parallel solution and solid phase synt...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2008-03, Vol.18 (6), p.1869-1873
Hauptverfasser:	Moree, Wilna J., Kataoka, Ken-ichiro, Ramirez-Weinhouse, Michele M., Shiota, Tatsuki, Imai, Minoru, Tsutsumi, Takaharu, Sudo, Masaki, Endo, Noriaki, Muroga, Yumiko, Hada, Takahiko, Fanning, Dewey, Saunders, John, Kato, Yoshinori, Myers, Peter L., Tarby, Christine M.
Format:	Artikel
Sprache:	eng
Schlagworte:	Antagonist Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Calcium - metabolism CCR2b Cells, Cultured Chemokine Chemokine CCL2 - metabolism Chemotaxis - drug effects Chromatography, High Pressure Liquid Fluorescence Humans Kidney - cytology Kidney - drug effects Kidney - metabolism Medical sciences Molecular Structure Monocytes - drug effects Monocytes - metabolism Pharmacology. Drug treatments Pyrrolidines - chemical synthesis Pyrrolidines - pharmacology Receptors, CCR2 - antagonists & inhibitors Receptors, CCR2 - metabolism Structure-Activity Relationship Transfection
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