Title of article
Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: Increased receptor specificity and in vivo activity
Author/Authors
Karsten Schnatbaum، نويسنده , , Elsa Locardi، نويسنده , , Dirk Scharn، نويسنده , , Klaus-Uwe Richter، نويسنده , , Heiko Hawlisch، نويسنده , , Jochen Knolle، نويسنده , , Thomas Polakowski، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
5
From page
5088
To page
5092
Abstract
A new class of peptidomimetic C5a receptor antagonists characterized by C-terminal amino acids with hydrophobic side chains is presented. Systematic optimization of the first hits led to JPE1375 (36), which was intensively characterized in vitro and in vivo. Compound 36 exhibits high microsomal stability and receptor specificity and is highly active in an immune complex mediated peritonitis model (reverse passive Arthus reaction) in mice.
Keywords
C5a receptor , Antagonist
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797335
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