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Kinetic target guided synthesis for the identification of macrophage migration inhibitory factor inhibitors (MIF)

Marzinzik, Andreas and Voegtle, Markus and Rondeau, Jean-Michel and Billich, Andreas and Pelle, Xavier and Manetsch, Roman and Monastyrskyi, Andrii (2014) Kinetic target guided synthesis for the identification of macrophage migration inhibitory factor inhibitors (MIF). Thesis.

Abstract

Several fragment based approaches have been established to identify fragments with good ligand efficiencies, but fail to provide insights into efficient fragment linkage, making the drug discovery process complicated. Herein, we report the applicaation of a novel drug discovery approach that generates biol. active compds., known as kinetic target guided synthesis (TGS). An 1,4 dipolar cycloaddition reaction between azides and alkynes was successfully employed for MIF templated screening to identify novel inhibitors of migration inhibitory factor inhibitors (MIF).

Item Type: Article
Keywords: Taget guided synthesis Macrophage migration inhibitory factor
Date Deposited: 18 May 2016 23:45
Last Modified: 18 May 2016 23:45
URI: https://oak.novartis.com/id/eprint/21010

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