Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10595433 | Bioorganic & Medicinal Chemistry Letters | 2013 | 4 Pages |
Abstract
Syntheses and biological evaluation of novel SRT1720 derivatives are described in search for new candidates of SIRT1 activator. Several parts of the SRT1720 structure, including piperazine moiety, quinoxaline ring on the amide group, and position of the amide function, were modified, and the assay results indicated that transfer of the ortho amide-substituent regarding to the imidazo[1,2-b]thiazole core onto the meta position resulted in improvement of SIRT1 activation ability. Modeling analyses of SRT1720 and the most potent derivative bound to model complex of SIRT1 with peptide substrate were also performed.
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Authors
Yuji Matsuya, Yuta Kobayashi, Sayumi Uchida, Yukihiro Itoh, Hideyuki Sawada, Takayoshi Suzuki, Naoki Miyata, Kenji Sugimoto, Naoki Toyooka,