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. 2011 Aug 15;21(16):4762-7.
doi: 10.1016/j.bmcl.2011.06.067. Epub 2011 Jun 29.

Optimization of a pyrazole hit from FBDD into a novel series of indazoles as ketohexokinase inhibitors

Xuqing Zhang  1 , Fengbing Song, Gee-Hong Kuo, Amy Xiang, Alan C Gibbs, Marta C Abad, Weimei Sun, Lawrence C Kuo, Zhihua Sui
Affiliations

Optimization of a pyrazole hit from FBDD into a novel series of indazoles as ketohexokinase inhibitors

Xuqing Zhang et al. Bioorg Med Chem Lett. .

Abstract

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.

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