Synthesis and SAR studies of 3, 6-disubstituted indazole derivatives as potent hepcidin production inhibitors. Issue 10 (15th May 2017)

• Record Type: Journal Article
• Authors: Fukuda, Takeshi; Ueda, Kenjiro; Ishiyama, Takashi; Goto, Riki; Muramatsu, Sumie; Hashimoto, Masami; Watanabe, Kengo; Tanaka, Naoki
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 27:Issue 10(2017)
• Page Start: 2148
• Page End: 2152
• Publication Date: 2017-05-15
• Subjects: Hepcidin -- Anemia of chronic disease -- Indazole -- Phenol -- Intraperitoneal administration; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2017.03.056
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: Hepcidin has emerged as the central regulatory molecule of systemic iron homeostasis. Inhibition of hepcidin could be a strategy favorable to treating anemia of chronic disease (ACD). We report herein the synthesis and structure-activity relationships (SARs) of a series of indazole compounds as hepcidin production inhibitors. The optimization study of compound1 led to a potent hepcidin production inhibitor45, which showed serum hepcidin lowering effects in a mouse IL-6 induced acute inflammatory model.