Title of article
SAR studies of 1,5-diarylpyrazole-based CCK1 receptor antagonists
Author/Authors
Laurent Gomez، نويسنده , , Michael D. Hack، نويسنده , , Kelly McClure، نويسنده , , Clark Sehon، نويسنده , , Liming Huang، نويسنده , , Magda Morton، نويسنده , , Lina Li، نويسنده , , Terrance D. Barrett، نويسنده , , Nigel Shankley، نويسنده , , J. Guy Breitenbucher، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
6
From page
6493
To page
6498
Abstract
A high throughput screening campaign revealed compound 1 as a potent antagonist of the human CCK1 receptor. Here, we report the syntheses and SAR studies of 1,5-diarylpyrazole analogs with various structural modifications of the alkane side chain of the molecule. The difference in affinity between the two enantiomers for the CCK1 receptor and the flexible nature of the linker led to the design of constrained analogs with increased potency.
Keywords
Pyrazole , cholecystokinin , Alkene analogs , CCK1
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798831
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