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

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.
Authors:
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  1. (J)
  2. (
Publication Date:
OSTI Identifier:
1025629
Resource Type:
Journal Article
Resource Relation:
Journal Name: Bioorg. Med. Chem. Lett.; Journal Volume: 21; Journal Issue: (16) ; 08, 2011
Research Org:
Advanced Photon Source (APS), Argonne National Laboratory (ANL), Argonne, IL (US)
Sponsoring Org:
INDUSTRY
Country of Publication:
United States
Language:
ENGLISH
Subject:
59 BASIC BIOLOGICAL SCIENCES; 60 APPLIED LIFE SCIENCES; CRYSTALLOGRAPHY; DRUGS; INDAZOLES; OPTIMIZATION; PYRAZOLES