University of Groningen
Development and application of novel scaffolds in drug discovery
Boltjes, André
DOI:
10.33612/diss.98161351
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Publication date: 2019
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Boltjes, A. (2019). Development and application of novel scaffolds in drug discovery: the MCR approach. Rijksuniversiteit Groningen. https://doi.org/10.33612/diss.98161351
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DEVELOPMENT AND APPLICATION OF NOVEL SCAFFOLDS IN DRUG DISCOVERY
The MCR approach
The research described in this thesis was carried out at the Department of Drug Design (Groningen Research Institute of Pharmacy, University of Groningen, The Netherlands) and was financially supported by the University of Groningen.
Printing of this thesis was financially supported by the University Library and the Graduate School of Science, Faculty of Science and Engineering, University of Groningen, The Netherlands
ISBN: 978-94-034-2005-9 (printed version) ISBN: 978-94-034-2004-2 (electronic version) Printing: Ipskamp printing, Enschede Cover design: André Boltjes
Cover Graphics: By pikisuperstar Source: Freepik
Copyright © 2019 André Boltjes. All rights are reserved. No part of this thesis may be reproduced or transmitted in any form or by any means without the prior permission in writing of the author.
Development and application
of novel scaffolds in Drug
Discovery
The MCR approach
Proefschrift
ter verkrijging van de graad van doctor aan de Rijksuniversiteit Groningen
op gezag van de
rector magnificus prof. dr. C. Wijmenga en volgens besluit van het College voor Promoties.
De openbare verdediging zal plaatsvinden op vrijdag 29 november 2019 om 14.30 uur
door
André Boltjes
geboren op 10 april 1984Promotores
Prof. dr. A.S.S. Dömling Prof. dr. F.J. Dekker
Beoordelingscommissie Prof. dr. R.V.A Orru Prof. dr. G.J. Poelarends Prof. dr. ir. A.J. Minnaard
Table of Contents
CHAPTER 1 GENERAL INTRODUCTION 1
CHAPTER 2 FRAGMENT BASED LIBRARY GENERATION FOR
THE DISCOVERY OF A PEPTIDOMIMETIC P53-MDM4 INHIBITOR
11
CHAPTER 3 UGI MULTICOMPONENT APPROACH TO
SYNTHESIZE SCHISTOSOMIASIS DRUG PRAZIQUANTEL
35
CHAPTER 4 UGI 4-CR SYNTHESIS OF γ- AND δ-LACTAMS
PROVIDING NEW ACCESS TO DIVERSE ENZYME INTERACTIONS, A PDB ANALYSIS
51
CHAPTER 5 Gd-TEMDO: DESIGN, SYNTHESIS AND MRI
APPLICATION 75
CHAPTER 6 THE GROEBKE-BLACKBURN-BIENAYMÉ
REACTION 97
CHAPTER 7 DIVERSE ONE-POT SYNTHESIS OF ADENINE
MIMETICS FOR BIOMEDICAL APPLICATIONS 189
CHAPTER 8 SUMMARY AND DISCUSSION 213
SAMENVATTING NEDERLANDSE SAMENVATTING 223
APPENDIX ACKNOWLEDGEMENTS 231
LIST OF PUBLICATIONS ABOUT THE AUTHOR
