Title of article
Synthesis, biological evaluation, and metabolic stability of acrylamide derivatives as novel CCR3 antagonists Original Research Article
Author/Authors
Ippei Sato، نويسنده , , Koichiro Morihira، نويسنده , , Hiroshi Inami، نويسنده , , Hirokazu Kubota، نويسنده , , Tatsuaki Morokata، نويسنده , , Keiko Suzuki، نويسنده , , Kazuki Ohno، نويسنده , , Yosuke Iura، نويسنده , , Aiko Nitta، نويسنده , , Takayuki Imaoka، نويسنده , , Toshiya Takahashi، نويسنده , , Makoto Takeuchi، نويسنده , , Mitsuaki Ohta، نويسنده , , Shin-ichi Tsukamoto، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2009
Pages
14
From page
5989
To page
6002
Abstract
Our laboratory has identified several acrylamide derivatives with potent CCR3 inhibitory activity. In the present study, we evaluated the in vitro metabolic stability (CLint; mL/min/kg) of these compounds in human liver microsomes (HLMs), and assessed the relationship between their structures and CLint values. Among the compounds identified, N-{(3R)-1-[(6-fluoro-2-naphthyl)methyl]pyrrolidin-3-yl}-2-[1-(2-hydroxybenzoyl)piperidin-4-ylidene]acetamide (30j) was found to be a potent inhibitor (IC50 = 8.4 nM) with a high metabolic stability against HLMs.
Keywords
Acrylamide derivatives , Allergic diseases , Clint , CCR3 antagonists
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2009
Journal title
Bioorganic and Medicinal Chemistry
Record number
1306267
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