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A series of novel indazole derivatives of Sirt 1 activator as osteogenic regulators
Authors:Masakazu Atobe  Natsumi Yamakawa  Yasuhiro Wada  Tokuhito Goto  Masashi Kawanishi  Takeshi Ito  Makoto Saito  Masahiro Takeda  Takanori Tabata  Hirokazu Arai
Affiliation:1. Laboratory for Medicinal Chemistry, Pharmaceutical Research Center, Asahi Kasei Pharma Corporation, 632-1 Mifuku, Izunokuni, Shizuoka 410-2321, Japan;2. Laboratory for Pharmacology, Pharmaceutical Research Center, Asahi Kasei Pharma Corporation, 632-1 Mifuku, Izunokuni, Shizuoka 410-2321, Japan
Abstract:A series of indazole derivatives were identified as Sirt 1 activators though high-throughput screening. Optimization of each substituent on the indazole ring led to the identification of compound 13. Compound 13 appeared to give the best Sirt 1 activity of the compounds tested and also showed osteogenesis activity in a cell assay. Sirt 1 activators are therefore potential candidates for the treatment of osteoporosis.
Keywords:Sirt 1  Osteoporosis  Osteogeneration  Indazole  HTS
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