Publikationen

Originalarbeiten

Development of Improved PPARβ/δ Inhibitors
P. M. Toth, S. Naruhn, V. F. S. Pape, S. M. A. Dörr, G. Klebe, R. Müller, W. E. Diederich
ChemMedChem 2012, 7, 159-170.
Abstract
High affinity PPARβ/δ-specific ligands with pure antagonistic or inverse agonistic properties
S. Naruhn, P. M. Toth, T. Adhikary, K. Kaddatz, V. Pape, S. Dörr, G. Klebe, S. Müller-Brüsselbach, W. E. Diederich
Mol Pharmacol 2011, 80, 828-838
Abstract
Fragment-based lead discovery: Screening and Optimising Fragments for Thermolysin Inhibition
L. Englert, K. Silber, H. Steuber, S. Brass, B. Over, H.-D. Gerber, A. Heine, W. E. Diederich, G. Klebe
ChemMedChem 2010, 5, 930-940.
Abstract
Pyrrolidine Derivatives as Plasmepsin Inhibitors: Binding Mode Analysis Assisted by Molecular Dynamics Simulations of a Highly Flexible Protein
T. Luksch, A. Blum, N. Klee, W. E. Diederich, C. A. Sotriffer, G. Klebe
ChemMedChem 2010, 5, 443-454
Abstract
Achiral Oligoamines as Versatile Tool for the Development of Aspartic Protease Inhibitors
A. Blum, J. Böttcher, B. Sammet, T. Luksch, A. Heine, G. Klebe, W. E. Diederich
Bioorganic Medicinal Chemistry 2008, 16, 8574-8586
Abstract
Targeting the Open Flap Conformation of HIV-1 Protease with Pyrrolidine-based Inhibitors
J. Böttcher, A. Blum, S. Dörr, A. Heine, W. E. Diederich, G. Klebe
ChemMedChem 2008, 3, 1337-1344
Abstract
Structural and Kinetic Analysis of Pyrrolidine-Based Inhibitors of the Drug-Resistant Ile84Val Mutant of HIV-1 Protease
J. Böttcher, A. Blum, A. Heine, W. E. Diederich, G. Klebe
Journal of Molecular Biology 2008, 383 (2), 347-357
Abstract
Computer-aided Design and Synthesis of non-peptidic Plasmepsin II and IV Inhibitors
T. Luksch, N.-S. Chan, S. Brass, C. A. Sotriffer, G. Klebe, W. E. Diederich
ChemMedChem 2008, 3, 1323-1336
Abstract
Structure-Guided Design of C₂-Symmetric HIV-1 Protease Inhibitors Based on a Pyrrolidine Scaffold
A. Blum, J. Böttcher, A. Heine, G. Klebe, W. E. Diederich
Journal of Medicinal Chemistry 2008, 51, 2078-2087
Abstract
KNOBLE: a knowledge-based approach for the design and synthesis of readily accessible small molecule chemical probes to test protein binding
C. Gerlach, M. Münzel, B. Baum, H.-D. Gerber, T. Craan, W. E. Diederich, Gerhard Klebe
Angewandte Chemie 2007, 119, 9265-9269
Angewandte Chemie International Edition 2007, 46, 9105-9109
Abstract
Synthesis of 2,3,4,7-tetrahydro-1H-azepines as privileged ligand scaffolds for the design of aspartic
protease inhibitors via a ring-closing metathesis approach
S. Brass, N.-S. Chan, C. Gerlach, T. Luksch, J. Böttcher, and W. E. Diederich
Journal of Organometallic Chemistry 2006, 691, 5406-5422
Abstract
Facile synthesis of substituted 2,3,4,7-tetrahydro-1H-azepines via ring-closing metathesis
S. Brass, H.-D. Gerber, S. Dörr, and W. E. Diederich
Tetrahedron 2006, 62, 1777-1786
Abstract
Formal Total Synthesis of (-)-Salicylihalamides A and B from D-Glucose and L-Rhamnose
T. Haack, K. Haack, W. E. Diederich, B. Blackman, S. Roy, S. Pusuluri, and G. I. GeorgJournal of Organic Chemistry 2005, 70, 7592-7604
Abstract
Formal Total Synthesis of (+)-Salicylihalamides A and B: A Combined Chiral Pool and RCM Strategy
K. Yang, B. Blackman, W. Diederich, P. T. Flaherty, C. J. Mossman, S. Roy, Y. M. Ahn, G. I. Georg
Journal of Organic Chemistry 2003, 68, 10030-10039
Abstract
Enantiospecific Formal Total Syntheses of (-)-Salicylihalamides A and B from D-Glucose and L-Rhamnose
K. Yang, T. Haack, B. Blackman, W. E. Diederich, S. Roy, S. Pusuluri, G. I. Georg
Organic Letters 2003, 5(21), 4007-4009.
Abstract
Synthesis and Structure of Novel 1λ⁴,2,6-Thiadiazines
W. E. Diederich und M. Haake
Journal of Organic Chemistry 2003, 68, 3817-3830.
Abstract

Übersichtsartikel

Proteases of Plasmodium falciparum as potential drug targets and inhibitors thereof
C. Wegscheid-Gerlach, H.-D. Gerber, W. E. Diederich
Current Topics in Medicinal Chemistry 2010, 10, 346-367.
Abstract
C₂-symmetric pyrrolidines derived from tartaric acids: versatile chiral building blocks for total synthesis, catalyst design, supramolecular and medicinal chemistry
A. Blum and W. E. Diederich
Current Organic Synthesis 2009, 6 (1), 38-53.
Abstract
Neue Konzepte zur Arzneistoffsuche und Synthese
W. Diederich, P. Haebel, A. Heine, K. Reuter, C. Sotriffer, G. Klebe
LaborPraxis 2004, 11, 24-26.

Vorträge

Einladungsvorträge

Auf der Suche nach neuen Wirkstoffen gegen AIDS und Malaria
Kolloquium im Rahmen des SFB 630 und der GDCh
Institut für Organische Chemie der Julius-Maximilians-Universität Würzburg, Würzburg, 02.07.2009
Protein-Ligand-Interaktionen - Ist die perfekte Passform wirklich alles?
Bayer-Schering Pharma AG, Berlin, 20.01.2009
Rational Design of C₂ -Symmetric Pyrrolidines as HIV-1 Protease Inhibitors
W.E. Diederich, A. Blum, J. Böttcher, G. Klebe
International Conference on Drug Design and Discovery for Developing Countries, Triest, Italien, 3.-5. Juli 2008
Design and Synthesis of C₂-symmetric Pyrrolidines as HIV Protease Inhibitors
W.E. Diederich, A. Blum, J. Böttcher, G. Klebe
New Frontiers in the Search of Bioactive Molecules: from Peptides to Drugs, 11^th Naples Workshop on Bioactive Peptides, Neapel, Italien, 24.-27. Mai 2008
Azazyklen als bevorzugte Ligandgerüste von Aspartyl-Protease-Inhibitoren – Design, Synthese und Strukturbestimmung
W.E. Diederich
Vortragsreihe Organische Chemie, Merck KGaA, Darmstadt, 25.01.2007
Design and Synthesis of tailor-made compound libraries via a knowledge-based approach - A case study
W.E. Diederich, C. Gerlach, A. Blum, J. Böttcher, S. Brass, T. Luksch, G. Klebe
Abstracts of Papers, 232^nd ACS National Meeting, San Francisco, CA, USA, September 2006

Sonstige Vorträge

Functionalized Pyrrolidines – A New Class of HIV-1 Protease Inhibitors
W.E. Diederich, A. Blum, J. Böttcher, G. Klebe
Frontiers in Medicinal Chemistry, Joint German-Swiss meeting on Medicinal Chemistry, Berlin, März 2007
Identification of azacycles as privileged ligand scaffolds for the design and synthesis of aspartic protease inhibitors
A. Blum, S. Brass, N.-S. Chan, W.E. Diederich
Abstracts of Papers, 232^nd ACS National Meeting, San Francisco, CA, USA, September 2006
Total Synthesis of the Salicylihalamides: Members of a new class of naturally occurring macrolides with promising cytotoxic activity
Deutsche Pharmazeutische Gesellschaft, Landesgruppe Hessen, Marburg, Februar 2003
Synthesis and structure of novel 1λ⁴,2,6-thiadiazines
19^th International Symposium on the Organic Chemistry of Sulfur (ISOCS-XIX), Sheffield, UK, Juni 2000