کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1369549 | 981782 | 2014 | 4 صفحه PDF | دانلود رایگان |
A series of 114 SIRT inhibitor candidates was assembled using ‘click chemistry’, by reacting two alkynes bearing 2-anilinobenzamide pharmacophore with 57 azide building blocks in the presence of Cu(I) catalyst. Screening identified two SIRT2-selective inhibitors, which were more SIRT2-selective than AGK2, a known SIRT2 inhibitor. These findings will be useful for further development of SIRT2-selective inhibitors.
To find novel SIRT2-selective inhibitors, we designed and prepared a library of SIRT inhibitor candidates derived from CuAAC reaction between propargyl 2-anilinobenzamides A and a series of azides B. Screening identified SIRT2-selective inhibitors A1B11 and A2B57, which were more SIRT2-selective than AGK2 (1), a known SIRT2 inhibitor. These findings will be useful in the further development of SIRT2-selective inhibitors.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 8, 15 April 2014, Pages 1871–1874