Title of article
The synthesis and structure–activity relationship studies of selective acetyl-CoA carboxylase inhibitors containing 4-(thiazol-5-yl)but-3-yn-2-amino motif: Polar region modifications
Author/Authors
Xiangdong Xu، نويسنده , , Moshe Weitzberg، نويسنده , , Robert F. Keyes، نويسنده , , Qun Li، نويسنده , , Rongqi Wang، نويسنده , , Xiaojun Wang، نويسنده , , Xiaolin Zhang، نويسنده , , Ernst U. Frevert، نويسنده , , Heidi S. Camp، نويسنده , , Bruce A. Beutel، نويسنده , , Hing L. Sham، نويسنده , , Yu Gui Gu، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
5
From page
1803
To page
1807
Abstract
The structure–activity relationship study focused on the polar region of the HTS hit A-80040 (1) producing several series of potent and selective ACC2 inhibitors. The SAR suggests a compact lipophilic pocket that does not tolerate polar and ionic groups. Replacement of the hydroxyurea group with isoxazoles improves ACC2 selectivity while maintaining potency. Variations at the propargylic site of 11a reduce ACC2 potency.
Keywords
ACC2 inhibitor , Polar region
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797938
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