- Synthesis and SAR studies of 3,6-disubstituted indazole derivatives as potent hepcidin production inhibitors
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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 compound 1 led to a potent hepcidin production inhibitor 45, which showed serum hepcidin lowering effects in a mouse IL-6 induced acute inflammatory model.
- Fukuda, Takeshi,Ueda, Kenjiro,Ishiyama, Takashi,Goto, Riki,Muramatsu, Sumie,Hashimoto, Masami,Watanabe, Kengo,Tanaka, Naoki
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p. 2148 - 2152
(2017/04/27)
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- 3-AMINOINDAZOLES
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Novel 3-aminoindazoles of formula (I) are SGK-inhibitors and can be used for treating SGK-related diseases and illnesses such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and renal diseases, and generally any type of fibroses and inflammatory processes.
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Page/Page column 78
(2008/06/13)
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- 6-Heteroaryl-pyrazolo[3,4-b]pyridines: Potent and selective inhibitors of Glycogen Synthase Kinase-3 (GSK-3)
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A series of 6-heteroaryl-pyrazolo[3,4-b]pyridines has been optimised to afford potent inhibitors of Glycogen Synthase Kinase-3 (GSK-3). These analogues display excellent selectivity over the closely related Cyclin Dependant Kinase-2 (CDK-2).
- Witherington, Jason,Bordas, Vincent,Gaiba, Alessandra,Naylor, Antoinette,Rawlings, Anthony D.,Slingsby, Brian P.,Smith, David G.,Takle, Andrew K.,Ward, Robert W.
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p. 3059 - 3062
(2007/10/03)
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