Synthesis, Biological Evaluation, and Automated Docking of Constrained Analogues of the Opioid Peptide H-Dmt-D-Ala-Phe-Gly-NH2 Using the 4- or 5-Methyl Substituted 4-Amino-1,2,4,5-tetrahydro-2-benzazepin-3-one Scaffold
De Wachter, R.; de Graaf, C.; Keresztes, A.; Vandormael, B.; Ballet, S.; Toth, G.; Rognan, D.; Tourwe, D., J. Med. Chem. 2011, 54, 6538-6547.
Read more
Solvent-free synthesis of hydrazones and their subsequent N-alkylation in a Ball-mill.
Nun, P.; Martin, C.; Martinez, J.; Lamaty, F., Tetrahedron 2011, 67, 8187-8194.
Read more
Design of Novel Neurokinin 1 Receptor Antagonists Based on Conformationally Constrained Aromatic Amino Acids and Discovery of a Potent Chimeric Opioid Agonist-Neurokinin 1 Receptor Antagonist.
Ballet, S.; Feytens, D.; Buysse, K.; Chung, N. N.; Lemieux, C.; Tumati, S.; Keresztes, A.; Van Duppen, J.; Lai, J.; Varga, E., J. Med. Chem. 2011, 54, 2467-2476.
Read more
Enantioselective Haloetherification by Asymmetric Opening of meso-Halonium Ions
U. Hennecke, C. H. Müller, R. Fröhlich, Org. Lett. 2011, 13, 860-863.
Read more
PK20, a new opioid-neurotensin hybrid peptide that exhibits central and peripheral antinociceptive effects.
Kleczkowska, P.; Kosson, P.; Ballet, S.; Van den Eynde, I.; Tsuda, Y.; Tourwé, D.; Lipkowski, A. W., Mol Pain 2010, 6, 86-92.
Read more
Sequential Double α-Arylation of N-Allylureas by Asymmetric Deprotonation and N→C Aryl Migration
D. J. Tetlow, U. Hennecke, J. Raftery, M. J. Waring, D. S. Clarke, J. Clayden, Org. Lett. 2010, 12, 5442-5445.
Read more
The Origin of the Conformational Preference of N,N'-diaryl-N,N'-dimethyl ureas
J. Clayden, U. Hennecke, M. A. Vincent, I. H. Hillier, M. Helliwell, Phys. Chem. Chem. Phys. 2010, 12, 15056-15064.
Read more
Novel multiple opioid ligands based on 4-aminobenzazepinone (Aba), azepinoindole (Aia) and tetrahydroisoquinoline (Tic) scaffolds.
Ballet, S.; Marczak, E. D.; Feytens, D.; Salvadori, S.; Sasaki, Y.; Abell, A. D.; Lazarus, L. H.; Balboni, G.; Tourwé, D., Bioorg. Med. Chem. Lett. 2010, 20, 1610-1613.
Read more
Crystal Structure of the T(6-4)C Lesion in Complex with a (6-4) DNA Photolyase and Repair of UV-Induced (6-4) and Dewar Photolesions
A. F. Glas, S. Schneider, M. J. Maul, U. Hennecke, T. Carell, Chem. Eur. J. 2009, 15, 10387-10396.
Read more
Synthesis and High-Resolution NMR Structure of a beta(3)-Octapeptide with and without a Tether Introduced by Olefin Metathesis.
Ebert, M. O.; Gardiner, J.; Ballet, S.; Abell, A. D.; Seebach, D., Helv. Chim. Acta 2009, 92, 2643-2658.
Read more
N to C Aryl Migration in Lithiated Carbamates: alpha-Arylation of Benzylic Alcohols
J. Clayden, W. Farnaby, D. M. Grainger, U. Hennecke, M. Mancinelli, D. J. Tetlow, I. H. Hillier, M. A. Vincent, J. Am. Chem. Soc. 2009, 131, 3410-3411.
Read more
α-Arylation of Cyclic Amines by Aryl Transfer in Lithiated Ureas
R. Bach, J. Clayden, U. Hennecke, Synlett 2009, 421-424.
Read more