Literature DB >> 24418813

First enzymatic hydrolysis/thio-Michael addition cascade route to synthesis of AChE inhibitors.

Emilia Oueis1, Florian Nachon, Cyrille Sabot, Pierre-Yves Renard.   

Abstract

The irreversible Michael addition of thiols to acrylamides is reported as a new tool for the kinetic target-guided synthesis. In an unprecedented enzymatic hydrolysis/thio-Michael addition procedure, potent and selective acetylcholinesterase inhibitors are assembled by the enzyme using both its esterasic and templating ability.

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Year:  2014        PMID： 24418813     DOI： 10.1039/c3cc48871c

Source DB:  PubMed          Journal:  Chem Commun (Camb)        ISSN： 1359-7345            Impact factor:   6.222


  6 in total

1.  A fluorescent target-guided Paal-Knorr reaction.

Authors:  Sachin B Wagh; Vladimir Maslivetc; James J La Clair; Alexander Kornienko
Journal:  RSC Adv       Date:  2020-10-07       Impact factor: 4.036

Review 2.  Protein-Templated Fragment Ligations-From Molecular Recognition to Drug Discovery.

Authors:  Mike Jaegle; Ee Lin Wong; Carolin Tauber; Eric Nawrotzky; Christoph Arkona; Jörg Rademann
Journal:  Angew Chem Int Ed Engl       Date:  2017-05-31       Impact factor: 15.336

3.  Proteintemplat-gesteuerte Fragmentligationen - von der molekularen Erkennung zur Wirkstofffindung.

Authors:  Mike Jaegle; Ee Lin Wong; Carolin Tauber; Eric Nawrotzky; Christoph Arkona; Jörg Rademann
Journal:  Angew Chem Weinheim Bergstr Ger       Date:  2017-05-31

4.  Optimized Inhibitors of MDM2 via an Attempted Protein-Templated Reductive Amination.

Authors:  Ramon van der Vlag; M Yagiz Unver; Tommaso Felicetti; Aleksandra Twarda-Clapa; Fatima Kassim; Cagdas Ermis; Constantinos G Neochoritis; Bogdan Musielak; Beata Labuzek; Alexander Dömling; Tad A Holak; Anna K H Hirsch
Journal:  ChemMedChem       Date:  2019-12-12       Impact factor: 3.466

5.  Protein-Templated Hit Identification through an Ugi Four-Component Reaction*.

Authors:  Federica Mancini; M Yagiz Unver; Walid A M Elgaher; Varsha R Jumde; Alaa Alhayek; Peer Lukat; Jennifer Herrmann; Martin D Witte; Matthias Köck; Wulf Blankenfeldt; Rolf Müller; Anna K H Hirsch
Journal:  Chemistry       Date:  2020-09-30       Impact factor: 5.236

6.  Irreversible inhibitors of the 3C protease of Coxsackie virus through templated assembly of protein-binding fragments.

Authors:  Daniel Becker; Zuzanna Kaczmarska; Christoph Arkona; Robert Schulz; Carolin Tauber; Gerhard Wolber; Rolf Hilgenfeld; Miquel Coll; Jörg Rademann
Journal:  Nat Commun       Date:  2016-09-28       Impact factor: 14.919
  6 in total

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