A series of novel indazole derivatives of Sirt 1 activator as osteogenic regulators. Issue 21 (1st November 2017)

• Record Type: Journal Article
• Authors: Atobe, Masakazu; Yamakawa, Natsumi; Wada, Yasuhiro; Goto, Tokuhito; Kawanishi, Masashi; Ito, Takeshi; Saito, Makoto; Takeda, Masahiro; Tabata, Takanori; Arai, Hirokazu
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 27:Issue 21(2017)
• Page Start: 4828
• Page End: 4831
• Publication Date: 2017-11-01
• Subjects: Sirt 1 -- Osteoporosis -- Osteogeneration -- Indazole -- HTS; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2017.09.049
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: 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 compound13. Compound13 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.