Title of article
Potent antagonists of the CCR2b receptor. Part 3: SAR of the (R)-3-aminopyrrolidine series
Author/Authors
Wilna J. Moree، نويسنده , , Ken-ichiro Kataoka، نويسنده , , Michele M. Ramirez-Weinhouse، نويسنده , , Tatsuki Shiota، نويسنده , , Minoru Imai، نويسنده , , Takaharu Tsutsumi، نويسنده , , Masaki Sudo، نويسنده , , Noriaki Endo، نويسنده , , Yumiko Muroga، نويسنده , , Takahiko Hada، نويسنده , , Dewey Fanning، نويسنده , , John Saunders، نويسنده , , Yoshinori Kato، نويسنده , , Peter L. Myers، نويسنده , , Christine M. Tarby، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
5
From page
1869
To page
1873
Abstract
SAR studies were conducted around lead compound 1 using high-throughput parallel solution and solid phase synthesis. Our lead optimization efforts led to the identification of several CCR2b antagonists with potent activity in both binding and functional assays [Compound 71 CCR2b Binding IC50 3.2 nM; MCP-1-Induced Chemotaxis IC50 0.83 nM; Ca2+ Flux IC50 7.5 nM].
Keywords
CCR2b , chemokine , Antagonist
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799263
Link To Document