1254069-40-3Relevant academic research and scientific papers
Optimization of a pyrazole hit from FBDD into a novel series of indazoles as ketohexokinase inhibitors
Zhang, Xuqing,Song, Fengbing,Kuo, Gee-Hong,Xiang, Amy,Gibbs, Alan C.,Abad, Marta C.,Sun, Weimei,Kuo, Lawrence C.,Sui, Zhihua
, p. 4762 - 4767 (2011/09/16)
A series of indazoles have been discovered as KHK inhibitors from a pyrazole hit identified through fragment-based drug discovery (FBDD). The optimization process guided by both X-ray crystallography and solution activity resulted in lead-like compounds with good pharmaceutical properties.
INDAZOLE COMPOUNDS USEFUL AS KETOHEXOKINASE INHIBITORS
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, (2011/11/06)
The present invention is directed to substituted indazole compounds, pharmaceutical compositions of these compounds and methods of use thereof. The compounds of the present invention are ketohexokinase (KHK) inhibitors, useful for treating or ameliorating a KHK mediated metabolic disorders and/or diseases such as obesity, Type II diabetes mellitus and Metabolic Syndrome X.
Electron density guided fragment-based lead discovery of ketohexokinase inhibitors
Gibbs, Alan C.,Abad, Marta C.,Zhang, Xuqing,Tounge, Brett A.,Lewandowski, Francis A.,Struble, Geoffrey T.,Sun, Weimei,Sui, Zhihua,Kuo, Lawrence C.
, p. 7979 - 7991 (2011/03/18)
A fragment-based drug design paradigm has been successfully applied in the discovery of lead series of ketohexokinase inhibitors. The paradigm consists of three iterations of design, synthesis, and X-ray crystallographic screening to progress low molecula
