Literature DB >> 21767952

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

Xuqing Zhang1, Fengbing Song, Gee-Hong Kuo, Amy Xiang, Alan C Gibbs, Marta C Abad, Weimei Sun, Lawrence C Kuo, Zhihua Sui.   

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.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID： 21767952     DOI： 10.1016/j.bmcl.2011.06.067

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  4 in total

1.  Computational chemistry at Janssen.

Authors:  Herman van Vlijmen; Renee L Desjarlais; Tara Mirzadegan
Journal:  J Comput Aided Mol Des       Date:  2016-12-19       Impact factor: 3.686

2.  3-substituted indazoles as configurationally locked 4EGI-1 mimetics and inhibitors of the eIF4E/eIF4G interaction.

Authors:  Revital Yefidoff-Freedman; Ting Chen; Rupam Sahoo; Limo Chen; Gerhard Wagner; Jose A Halperin; Bertal H Aktas; Michael Chorev
Journal:  Chembiochem       Date:  2014-01-23       Impact factor: 3.164

3.  Synthesis of substituted 2H-benzo[e]indazole-9-carboxylate as a potent antihyperglycemic agent that may act through IRS-1, Akt and GSK-3β pathways.

Authors:  Gaurav Taneja; Chandra Prakash Gupta; Shachi Mishra; Rohit Srivastava; Neha Rahuja; Arun Kumar Rawat; Jyotsana Pandey; Anand P Gupta; Natasha Jaiswal; Jiaur R Gayen; Akhilesh K Tamrakar; Arvind Kumar Srivastava; Atul Goel
Journal:  Medchemcomm       Date:  2016-11-15       Impact factor: 3.597

Review 4.  The Role of Fructose in Non-Alcoholic Steatohepatitis: Old Relationship and New Insights.

Authors:  Alessandro Federico; Valerio Rosato; Mario Masarone; Pietro Torre; Marcello Dallio; Mario Romeo; Marcello Persico
Journal:  Nutrients       Date:  2021-04-16       Impact factor: 5.717
  4 in total

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