2014 and Earlier

Boldron, C.; Besse, A.; Bordes, M.-F.; Tissandié, S.; Yvon, X.; Gau, B.; Badorc, A.; Rousseaux, T.; Barré, G.; Meneyrol, J.; Zech, G.; Nazaré, M.; Fossey, V.; Pflieger, A.-M.; Bonnet-Lignon, S.; Millet, L.; Briot, C.; Dol, F.; Herault, J.-P.; Savi, P.; Lassalle, G. Y.; Delesque, N.; Herbert, J.-M.; Bono, F. N-[6-(4-butanoyl-5-methyl-1H-pyrazol-1-yl)pyridazin-3-yl]-5-chloro-1-[2-(4-methyl-piperazin-1-yl)-2-oxoethyl]-1H-indole-3-carboxamide (SAR216471), a Novel Intravenous and Oral, Reversible and Directly Acting P2Y12 Antagonist. J. Med. Chem. 2014, 57, 7293-7316. doi.org/10.1021/jm500588w

Wilde, F.; Specker, E.; Neuenschwander, M.; Nazaré, M.; Bodtke, A.; Link, A. Tractable synthesis of multipurpose screening compounds with under-represented molecular features for an open access screening platform. Mol. Divers. 2014, 18, 483-495. doi.org/10.1007/s11030-014-9518-6

Zech, G.; Hessler, G.; Evers, A.; Weiss, T.; Florian, P.; Just, M.; Czech, J.; Czechtizky, W.; Görlitzer, J.; Ruf, S.; Kohlmann, M.; Nazaré, M. Identification of high-affinity P2Y₁₂ antagonists based on a phenylpyrazole glutamic acid piperazine backbone. J. Med. Chem. 2012, 55, 8615-8629. doi.org/10.1021/jm300771j.

Kozian, D. H.; Evers, A.; Florian, P.; Wonerow, P.; Joho, S.; Nazaré, M. Selective non-lipid modulator of LPA5 activity in human platelets. Bioorg. Med. Chem. Lett., 2012, 22, 5239-5243. doi.org/10.1016/j.bmcl.2012.06.057.

Nazaré, M.; Matter, H.; Will, D. W.; Wagner, M.; Urmann, M.; Czech, J.; Schreuder, H.; Bauer, A.; Ritter, K.; Wehner, V. Fragment Deconstruction of Small, Potent Factor Xa Inhibitors: Exploring the Superadditivity Energetics of Fragment Linking in Protein–Ligand Complexes., Angew. Chem. Int. Ed., 2012, 124, 929-935. doi.org/10.1002/ange.201107091.

Alonso, J.; Halland, N.; Nazaré, M.; R'kyek, O.; Urmann, M.; Lindenschmidt, A.; A Direct, Regioselective Palladium-Catalyzed Synthesis of N-Substituted Benzimidazoles and Imidazopyridines. Eur. J. Org. Chem., 2011, 234-237. doi.org/10.1002/ejoc.201001423.

R'kyek, O.; Halland, N.; Lindenschmidt, A.; Alonso, J.; Lindemann, P.; Urmann, M.; Nazaré, M., A General Palladium-Catalyzed Sonogashira Coupling of Aryl and Heteroaryl Tosylates. Chem. Eur. J., 2010, 16, 9986-9989. doi.org/10.1002/chem.201001524.

Halland, N.; Nazaré, M.; R'kyek, O.; Alonso, J.; Urmann, M.; Lindenschmidt, A., A General and Mild Palladium-Catalyzed Domino Reaction for the Synthesis of 2H-Indazoles., Angew. Chem. Int. Ed.; 2009, 48, 6879-6882. doi.org/10.1002/anie.200902323.

Matter, H.; Nazaré, M.; Guessregen, S.; Will, D. W.; Schreuder, H.; Bauer, A.; Urmann, M.; Ritter, K.; Wagner, M.; Wehner, V.; Evidence for C-Cl/C-Br...π interactions as an important contribution to protein-ligand binding affinity. Angew. Chem., Int. Ed. 2009, 48, 2911-2916 https://doi.org/10.1002/anie.200806219

Nazaré, M., Will, D. W.; Matter, H.; Schreuder, H.; Ritter, K.; Urmann, M.; Essrich, M.; Bauer, A.; Wagner, M.; Czech, J.; Lorenz M.; Laux, V.; Wehner, V., Probing the Subpockets of Factor Xa Reveals Two Binding Modes for Inhibitors Based on a 2-Carboxyindole Scaffold: A Study Combining Structure-Activity Relationship and X-ray Crystallography, J. Med. Chem. 2005, 48, 4511-4525. doi.org/10.1021/jm0490540

Matter, H.; Will, D. W.; Nazaré, M.; Schreuder, H.; Laux, V.; Wehner, V.; Structural Requirements for Factor Xa Inhibition by 3-Oxybenzamides with Neutral P1 Substituents: Combining X-ray Crystallography, 3D-QSAR and Tailored Scoring Functions. J. Med. Chem. 2005, 48, 3290-3312. doi.org/10.1021/jm049187l

Nazaré, M.; Schneider, C.; Lindenschmidt, A.; Will, D. W.; A flexible, palladium-catalyzed indole and azaindole synthesis by direct annulation of chloroanilines and chloroaminopyridines with ketones. Angew. Chem., Int. Ed. 2004, 43, 4526-4528. doi.org/10.1002/anie.200460122

Nazaré, M.; Essrich, M.; W. Will, D. W.; Matter, H.; Ritter, K.; Urmann, M.; Bauer, A.; Schreuder, H.; Czech, J.; Lorenz, M.; Laux, V.; Wehner, V. Novel Factor Xa Inhibitors Based on a 2-Carboxyindole Scaffold: SAR of P4 Substituents in Combination with a Neutral P1 Ligand. Bioorg. Med. Chem. Lett. 2004, 14, 4197-4201. doi.org/10.1016/j.bmcl.2004.06.019

Nazaré, M.; Essrich, M.; W. Will, D. W.; Matter, H.; Ritter, K.; Urmann, M.; Bauer, A.; Schreuder, H.; Dudda, A.; Czech, J.; Lorenz, M.; Laux, V.; Wehner, V.; Factor Xa Inhibitors Based on a 2-Carboxyindole Scaffold: SAR of Neutral P1 Substituents. Bioorg. Med. Chem. Lett. 2004, 14, 4191-4195. doi.org/10.1016/j.bmcl.2004.06.020

Nazaré, M.; Matter, H.; Klingler, O.; Al-Obeidi, F.; Schreuder, H.; Zoller, G.; Czech, J.; Lorenz, M.; Dudda, A.; Peyman, A.; Nestler, H.-P.; Urmann, M.; Bauer, A.; Laux, V.; Wehner, V.; Will, D. W.;Novel Factor Xa Inhibitors Based on a Benzoic Acid Scaffold and Incorporating a Neutral P1 Ligand. Bioorg. Med. Chem. Lett. 2004, 14, 2801-2805. doi.org/10.1016/j.bmcl.2004.03.059