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1. In-vitro test system for the evaluation of cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) inhibitors based on a single HPLC run with UV detection using bovine aortic coronary endothelial cells (BAECs)

Author

G. Dannhardt and H. Ulbrich

Subjects
Blotting, Western, Immunology, Drug Evaluation, Preclinical, Aorta, Thoracic, In Vitro Techniques, High-performance liquid chromatography, Lipoxygenase, Diclofenac, medicine, Animals, Cyclooxygenase Inhibitors, Lipoxygenase Inhibitors, IC50, Chromatography, High Pressure Liquid, Pharmacology, Cyclooxygenase 2 Inhibitors, biology, Chemistry, Molecular biology, Isoenzymes, Kinetics, Meloxicam, Biochemistry, Cyclooxygenase 2, Prostaglandin-Endoperoxide Synthases, Polyclonal antibodies, Cyclooxygenase 1, biology.protein, Tetradecanoylphorbol Acetate, Aceclofenac, Cattle, Spectrophotometry, Ultraviolet, Endothelium, Vascular, Cyclooxygenase, medicine.drug
Abstract

Objective and Design: The aim of this study was to develop a new, whole-cell test system which is easy to handle and requires a standard equipment for the parallel screening of COX-1 and COX-2 inhibitors.¶Materials: Bovine aortic endothelial cells (BAECs).¶Treatment and methods: Unstimulated bovine aortic coronary endothelial cells (BAECs) were used as a source of COX-1 and BAECs pretreated with ASA (100 μM) and activated with phorbol myristate acetate (PMA) were used as a source of COX-2. The time- and concentration-dependent induction of COX-2 expression in the BAECs was evaluated by a kinetic profile (HPLC analysis) and detected by Western-Blot analysis using polyclonal antibodies against COX-1 and COX-2.¶Results: In BAECs, diclofenac and meloxicam showed balanced inhibition of COX-1 (IC50: 0.01/0.4 μM) and COX-2 (IC50: 0.03/0.6 μM). Indomethacin inhibited COX-1 more potently than COX-2 (IC50: 0.008/0.04 μM). Aceclofenac inhibited COX-2 more potently than COX-1 (IC50: 3.0/7.3 μM). DFU and Cl-SC57666 [16] inhibited COX-2 (IC50: 0.04/0.001 μM) highly selectively but did not inhibit COX-1 (IC50: >100 μM).¶Conclusions: In summary an assay has been developed, for the determination of IC50-values for inhibitors of COX-1/2 on cells of the same origin, in line with values in the literature. Moreover, new insights have been gained into the relationship of COX-1/2 and lipoxygenase pathways in BAECs by detecting 15- and 12-HETE: Inhibition of COX-1 by the NSAIDs mostly resulted in an enhancement of 15-HETE and 12-HETE release. In contrast inhibition of COX-2 decreased 15-HETE release.¶

Published
2001
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3. A novel series of 2-carboxytetrahydroquinolines provides new insights into the eastern region of glycine site NMDA antagonists

Author

G, Dannhardt, M, von Gruchalla, B K, Kohl, and C G, Parsons

Subjects
Male, Binding Sites, Patch-Clamp Techniques, Cell Membrane, Glycine, Brain, Kynurenic Acid, Receptors, N-Methyl-D-Aspartate, Rats, Rats, Sprague-Dawley, Radioligand Assay, Ethers, Cyclic, Quinolines, Animals, Urea, Excitatory Amino Acid Antagonists
Abstract

A series of potent 4-substituted tetrahydroquinolines has been synthesized and biologically tested in order to refine the eastern region of the pharmacophore model for glycine site NMDA antagonists concerning the assessment of lipophilicity, flexibility, and hydrogen bonding. Displacement studies on rat cortical membranes using [3H]-5,7-dichlorokynurenic acid as a radioligand indicated that binding affinities are markedly enhanced when additional hydrogen-accepting groups are introduced into the eastern region of the 2-carboxytetrahydroquinolines. Among the most potent ligands were some urea, sulfonylurea, and crown ether compounds as interesting leads for new diagnostics, especially for the evaluation of PET tracers, which allow biodistribution studies and NMDA receptor studies in the living organism.

Published
2000

4. Effect of flavonol derivatives on the carrageenin-induced paw edema in the rat and inhibition of cyclooxygenase-1 and 5-lipoxygenase in vitro

Author

A M, Sobottka, W, Werner, G, Blaschke, W, Kiefer, U, Nowe, G, Dannhardt, E E, Schapoval, E P, Schenkel, and G K, Scriba

Subjects
Flavonoids, Flavonols, Foot, Anti-Inflammatory Agents, Membrane Proteins, Carrageenan, Rats, Isoenzymes, Inhibitory Concentration 50, Prostaglandin-Endoperoxide Synthases, Cyclooxygenase 1, Animals, Edema, Cattle, Cyclooxygenase Inhibitors, Lipoxygenase Inhibitors, Enzyme Inhibitors, Rats, Wistar
Abstract

Alkoxyflavonols were synthesized by the Algar-Flynn-Oyamada (AFO) cyclization of chalcones. Hydroxyflavonols were prepared by dealkylation of methoxyflavonols by refluxing in hydroiodic acid. The alkoxyflavonols 3-hydroxy-2-(2,3,4-trimethoxyphenyl)-4H-chromen-4-one (6), 2-(4-ethoxyphenyl)-3-hydroxy-4H-chromen-4-one (7), 2-(4-butoxyphenyl)-3-hydroxy-4H-chromen-4-one (10), and 2-(3-n-butoxyphenyl)-3-hydroxy-4H-chromen-4-one (11) as well as the trihydroxy derivative 3-hydroxy-2-(3,4,5-trihydroxyphenyl)-4H-chromen-4-one (18) displayed high anti-inflammatory activity in carrageenin-induced rat paw edema. Additionally, the inhibition of enzymes of the arachidonic acid cascade by the derivatives was investigated in vitro. In contrast to the natural compound quercetin, the compounds were more potent inhibiting cyclooxygenase-1 than 5-lipoxygenase except for 3-hydroxy-7-methoxy-2-(4-methoxyphenyl)-4H-chromen-4-one (5). No correlation between the anti-inflammatory activity in the rat paw edema test and the inhibition of 5-lipoxygenase or cyclooxygenase-1 could be observed. In conclusion, the present results suggest that other effects than inhibition of these enzymes of the arachidonic acid cascade are important for the anti-inflammatory activity of the investigated alkoxyflavonols.

Published
2000

5. Benzimidazoles as NMDA glycine-site antagonists: study on the structural requirements in 2-position of the ligand

Author

G, Dannhardt and B K, Kohl

Subjects
Cerebral Cortex, Male, Rats, Sprague-Dawley, Binding Sites, Indoles, Molecular Structure, Glycine, Animals, Benzimidazoles, Binding, Competitive, Excitatory Amino Acid Antagonists, Receptors, N-Methyl-D-Aspartate, Rats
Abstract

A series of different substituted benzimidazole derivatives has been synthesized and evaluated for the ability to displace [3H]MDL-105,519 to rat cortical membranes. Two benzimidazole-2-carboxylic acids 9 b and 9 c, in this substitution pattern not yet described as glycine antagonists, showed IC50 values of 0.89 microM (9 b) and 38.0 microM (9 c). Replacement of the carboxylate function in 2-position by a sulfonic acid moiety appreciably increased solubility, but decreased the affinity giving evidence for the strong need of the carboxylate group within the ligand. Further structure-activity studies using benzimidazole-2-one derivatives with an acetic acid moiety adjacent to a ring nitrogen revealed new insights into the importance of amide functionalities within the heterocycle for the affinity of antagonist glycine-site ligands.

Published
2000

6. [COX-2 inhibitors: current status and outlook]

Author

G, Dannhardt and L, Hahn

Subjects
Isoenzymes, Cyclooxygenase 2 Inhibitors, Cyclooxygenase 2, Prostaglandin-Endoperoxide Synthases, Humans, Membrane Proteins, Cyclooxygenase Inhibitors
Published
2000

7. D

Author

Franz von Bruchhausen, Eberhard Hackenthal, Siegfried Ebel, Ulrike Holzgrabe, August Wilhelm Frahm, M. Albinus, G. Amschler, E. von Angerer, null Arras-Reiter, P. Barth, W. Barthel, K. Bauer, P. Bauer, I. Baumann, J. Beckmann, W. Beil, J. Reitz, K. Binder, F. Bossle, F. Bracher, H. Bräunlich, E. Bretschneider, R. Brigelius-Flohé, K. Brinkmann, F. von Bruchhausen, A. Rüge, W. Christ, M. Cimbollek, R. Daniels, G. Dannhardt, H. Duchstein, S. Ebel, K. Eger, P. Eichhorn, U. Eiben, T. Erker, P. Felfe, A. Frahm, M. Frahm, V. Franke, K. Freundt, D. Geffken, U. Geis, E. Glusa, B. Göber, P. Gobina, W. Golder, M. Goppelt­Strübe, K. Götte, E. Gottstein, G. Greif, A. Grisk, M. Grosam, H. Gustmann, M. Gütschow, E. Hackenthal, A. Häfner, B. Haluszczynski, A. Harder, H. Häusler, D. Heber, M. Heidenreich, G. Heinemeyer, E. Heller, D. von Herrath, J. Hilfenhaus, H. Hoffmann, U. Hoffmann-Schollmayer, B. Hofmann, C. Holpert, U. Holzgrabe, U. Hübner-Steiner, M. Hug, E. Inkmann, A. Jördens, J. Jürgens, B. Kaiser, D. Kalbhen, H. Kemmler, P. Kisser, D. Kleinsorge, C. Klett, S. Klett, M. Klingmüller, H. Klöcking, A. Kramer, B. Krammer, M. Kreher, M. Krüger, M. Kuhn, D. Landsiedel-Maier, P. Lauven, J. Lehmann, M. Lehner, D. Leopoldt, A. Maurer, W. Meindl, K. Menges, P. Mes­singer, F. Meyer, W. Meyerhof, R. Morgenstern, U. Mühlhans, A. Müller, C. Müller, K. Müller, A. Mülsch, C. Nachtsheim, M. Neugebauer, W. Neupert, P. Nickel, P. Nuhn, B. Nürnberg, H. Oelschläger, J. Oertel, M. Oettel, R. Ott, T. Ott, T. Otzen, P. Pachaly, H. Pelzer, K. Petersen, R. Pick, M. Pickert, A. Pies, H. Priewer, O. Queckenberg, G. Radau, E. Reimann, J. Remien, M. Reuß, W. Reuß, J. Richter, P. Richter, K. Riecke, H. Rommelspacher, U. Rose, G. Roth, D. Rothley, G. Rücker, J. Schäfer, J. Schantl, H. Schlager, H. Schleinitz, W. Schlichter, M. Schmauß, H. Schmidhammer, G. Schmidt, T. Schmidt, H. Schmitt, J. Sehräder, T. Schulz, H. Schwilden, M. Serke, G. Skopp, G. Skorka, K. Smolinka, U. Speck, M. Spohn, R. Stahlmann, J. Stasch, C. Steffen, H. Stein, J. Steinmeyer, K. Stiefvater, G. Strippel, K. Surborg, U. Stürig, H. Szelényi, I. Szelényi, A. Täufel, R. Thieroff-Ekerdt, R. Troschütz, H. Ungeheuer, B. Unterhalt, E. Verspohl, S. Vogel, F. Volk, T. Vorwerk, J. Wallmann, H. Weber, M. Wenzel, M. Weyandt-Spangenberg, S. Wich, R. Wintersteiger, B. Wüst, and D. Youssef

Published
1999
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8. A

Author

Franz von Bruchhausen, Eberhard Hackenthal, Siegfried Ebel, Ulrike Holzgrabe, August Wilhelm Frahm, M. Albinus, G. Amschler, E. von Angerer, null Arras-Reiter, P. Barth, W. Barthel, K. Bauer, P. Bauer, I. Baumann, J. Beckmann, W. Beil, J. Reitz, K. Binder, F. Bossle, F. Bracher, H. Bräunlich, E. Bretschneider, R. Brigelius-Flohé, K. Brinkmann, F. von Bruchhausen, A. Rüge, W. Christ, M. Cimbollek, R. Daniels, G. Dannhardt, H. Duchstein, S. Ebel, K. Eger, P. Eichhorn, U. Eiben, T. Erker, P. Felfe, A. Frahm, M. Frahm, V. Franke, K. Freundt, D. Geffken, U. Geis, E. Glusa, B. Göber, P. Gobina, W. Golder, M. Goppelt­Strübe, K. Götte, E. Gottstein, G. Greif, A. Grisk, M. Grosam, H. Gustmann, M. Gütschow, E. Hackenthal, A. Häfner, B. Haluszczynski, A. Harder, H. Häusler, D. Heber, M. Heidenreich, G. Heinemeyer, E. Heller, D. von Herrath, J. Hilfenhaus, H. Hoffmann, U. Hoffmann-Schollmayer, B. Hofmann, C. Holpert, U. Holzgrabe, U. Hübner-Steiner, M. Hug, E. Inkmann, A. Jördens, J. Jürgens, B. Kaiser, D. Kalbhen, H. Kemmler, P. Kisser, D. Kleinsorge, C. Klett, S. Klett, M. Klingmüller, H. Klöcking, A. Kramer, B. Krammer, M. Kreher, M. Krüger, M. Kuhn, D. Landsiedel-Maier, P. Lauven, J. Lehmann, M. Lehner, D. Leopoldt, A. Maurer, W. Meindl, K. Menges, P. Mes­singer, F. Meyer, W. Meyerhof, R. Morgenstern, U. Mühlhans, A. Müller, C. Müller, K. Müller, A. Mülsch, C. Nachtsheim, M. Neugebauer, W. Neupert, P. Nickel, P. Nuhn, B. Nürnberg, H. Oelschläger, J. Oertel, M. Oettel, R. Ott, T. Ott, T. Otzen, P. Pachaly, H. Pelzer, K. Petersen, R. Pick, M. Pickert, A. Pies, H. Priewer, O. Queckenberg, G. Radau, E. Reimann, J. Remien, M. Reuß, W. Reuß, J. Richter, P. Richter, K. Riecke, H. Rommelspacher, U. Rose, G. Roth, D. Rothley, G. Rücker, J. Schäfer, J. Schantl, H. Schlager, H. Schleinitz, W. Schlichter, M. Schmauß, H. Schmidhammer, G. Schmidt, T. Schmidt, H. Schmitt, J. Sehräder, T. Schulz, H. Schwilden, M. Serke, G. Skopp, G. Skorka, K. Smolinka, U. Speck, M. Spohn, R. Stahlmann, J. Stasch, C. Steffen, H. Stein, J. Steinmeyer, K. Stiefvater, G. Strippel, K. Surborg, U. Stürig, H. Szelényi, I. Szelényi, A. Täufel, R. Thieroff-Ekerdt, R. Troschütz, H. Ungeheuer, B. Unterhalt, E. Verspohl, S. Vogel, F. Volk, T. Vorwerk, J. Wallmann, H. Weber, M. Wenzel, M. Weyandt-Spangenberg, S. Wich, R. Wintersteiger, B. Wüst, and D. Youssef

Published
1999
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9. H

Author

Franz von Bruchhausen, Eberhard Hackenthal, Siegfried Ebel, Ulrike Holzgrabe, August Wilhelm Frahm, M. Albinus, G. Amschler, E. von Angerer, null Arras-Reiter, P. Barth, W. Barthel, K. Bauer, P. Bauer, I. Baumann, J. Beckmann, W. Beil, J. Reitz, K. Binder, F. Bossle, F. Bracher, H. Bräunlich, E. Bretschneider, R. Brigelius-Flohé, K. Brinkmann, F. von Bruchhausen, A. Rüge, W. Christ, M. Cimbollek, R. Daniels, G. Dannhardt, H. Duchstein, S. Ebel, K. Eger, P. Eichhorn, U. Eiben, T. Erker, P. Felfe, A. Frahm, M. Frahm, V. Franke, K. Freundt, D. Geffken, U. Geis, E. Glusa, B. Göber, P. Gobina, W. Golder, M. Goppelt­Strübe, K. Götte, E. Gottstein, G. Greif, A. Grisk, M. Grosam, H. Gustmann, M. Gütschow, E. Hackenthal, A. Häfner, B. Haluszczynski, A. Harder, H. Häusler, D. Heber, M. Heidenreich, G. Heinemeyer, E. Heller, D. von Herrath, J. Hilfenhaus, H. Hoffmann, U. Hoffmann-Schollmayer, B. Hofmann, C. Holpert, U. Holzgrabe, U. Hübner-Steiner, M. Hug, E. Inkmann, A. Jördens, J. Jürgens, B. Kaiser, D. Kalbhen, H. Kemmler, P. Kisser, D. Kleinsorge, C. Klett, S. Klett, M. Klingmüller, H. Klöcking, A. Kramer, B. Krammer, M. Kreher, M. Krüger, M. Kuhn, D. Landsiedel-Maier, P. Lauven, J. Lehmann, M. Lehner, D. Leopoldt, A. Maurer, W. Meindl, K. Menges, P. Mes­singer, F. Meyer, W. Meyerhof, R. Morgenstern, U. Mühlhans, A. Müller, C. Müller, K. Müller, A. Mülsch, C. Nachtsheim, M. Neugebauer, W. Neupert, P. Nickel, P. Nuhn, B. Nürnberg, H. Oelschläger, J. Oertel, M. Oettel, R. Ott, T. Ott, T. Otzen, P. Pachaly, H. Pelzer, K. Petersen, R. Pick, M. Pickert, A. Pies, H. Priewer, O. Queckenberg, G. Radau, E. Reimann, J. Remien, M. Reuß, W. Reuß, J. Richter, P. Richter, K. Riecke, H. Rommelspacher, U. Rose, G. Roth, D. Rothley, G. Rücker, J. Schäfer, J. Schantl, H. Schlager, H. Schleinitz, W. Schlichter, M. Schmauß, H. Schmidhammer, G. Schmidt, T. Schmidt, H. Schmitt, J. Sehräder, T. Schulz, H. Schwilden, M. Serke, G. Skopp, G. Skorka, K. Smolinka, U. Speck, M. Spohn, R. Stahlmann, J. Stasch, C. Steffen, H. Stein, J. Steinmeyer, K. Stiefvater, G. Strippel, K. Surborg, U. Stürig, H. Szelényi, I. Szelényi, A. Täufel, R. Thieroff-Ekerdt, R. Troschütz, H. Ungeheuer, B. Unterhalt, E. Verspohl, S. Vogel, F. Volk, T. Vorwerk, J. Wallmann, H. Weber, M. Wenzel, M. Weyandt-Spangenberg, S. Wich, R. Wintersteiger, B. Wüst, and D. Youssef

Published
1999
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10. I

Author

Franz von Bruchhausen, Eberhard Hackenthal, Siegfried Ebel, Ulrike Holzgrabe, August Wilhelm Frahm, M. Albinus, G. Amschler, E. von Angerer, null Arras-Reiter, P. Barth, W. Barthel, K. Bauer, P. Bauer, I. Baumann, J. Beckmann, W. Beil, J. Reitz, K. Binder, F. Bossle, F. Bracher, H. Bräunlich, E. Bretschneider, R. Brigelius-Flohé, K. Brinkmann, F. von Bruchhausen, A. Rüge, W. Christ, M. Cimbollek, R. Daniels, G. Dannhardt, H. Duchstein, S. Ebel, K. Eger, P. Eichhorn, U. Eiben, T. Erker, P. Felfe, A. Frahm, M. Frahm, V. Franke, K. Freundt, D. Geffken, U. Geis, E. Glusa, B. Göber, P. Gobina, W. Golder, M. Goppelt­Strübe, K. Götte, E. Gottstein, G. Greif, A. Grisk, M. Grosam, H. Gustmann, M. Gütschow, E. Hackenthal, A. Häfner, B. Haluszczynski, A. Harder, H. Häusler, D. Heber, M. Heidenreich, G. Heinemeyer, E. Heller, D. von Herrath, J. Hilfenhaus, H. Hoffmann, U. Hoffmann-Schollmayer, B. Hofmann, C. Holpert, U. Holzgrabe, U. Hübner-Steiner, M. Hug, E. Inkmann, A. Jördens, J. Jürgens, B. Kaiser, D. Kalbhen, H. Kemmler, P. Kisser, D. Kleinsorge, C. Klett, S. Klett, M. Klingmüller, H. Klöcking, A. Kramer, B. Krammer, M. Kreher, M. Krüger, M. Kuhn, D. Landsiedel-Maier, P. Lauven, J. Lehmann, M. Lehner, D. Leopoldt, A. Maurer, W. Meindl, K. Menges, P. Mes­singer, F. Meyer, W. Meyerhof, R. Morgenstern, U. Mühlhans, A. Müller, C. Müller, K. Müller, A. Mülsch, C. Nachtsheim, M. Neugebauer, W. Neupert, P. Nickel, P. Nuhn, B. Nürnberg, H. Oelschläger, J. Oertel, M. Oettel, R. Ott, T. Ott, T. Otzen, P. Pachaly, H. Pelzer, K. Petersen, R. Pick, M. Pickert, A. Pies, H. Priewer, O. Queckenberg, G. Radau, E. Reimann, J. Remien, M. Reuß, W. Reuß, J. Richter, P. Richter, K. Riecke, H. Rommelspacher, U. Rose, G. Roth, D. Rothley, G. Rücker, J. Schäfer, J. Schantl, H. Schlager, H. Schleinitz, W. Schlichter, M. Schmauß, H. Schmidhammer, G. Schmidt, T. Schmidt, H. Schmitt, J. Sehräder, T. Schulz, H. Schwilden, M. Serke, G. Skopp, G. Skorka, K. Smolinka, U. Speck, M. Spohn, R. Stahlmann, J. Stasch, C. Steffen, H. Stein, J. Steinmeyer, K. Stiefvater, G. Strippel, K. Surborg, U. Stürig, H. Szelényi, I. Szelényi, A. Täufel, R. Thieroff-Ekerdt, R. Troschütz, H. Ungeheuer, B. Unterhalt, E. Verspohl, S. Vogel, F. Volk, T. Vorwerk, J. Wallmann, H. Weber, M. Wenzel, M. Weyandt-Spangenberg, S. Wich, R. Wintersteiger, B. Wüst, and D. Youssef

Published
1999
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11. C

Author

Franz von Bruchhausen, Eberhard Hackenthal, Siegfried Ebel, Ulrike Holzgrabe, August Wilhelm Frahm, M. Albinus, G. Amschler, E. von Angerer, null Arras-Reiter, P. Barth, W. Barthel, K. Bauer, P. Bauer, I. Baumann, J. Beckmann, W. Beil, J. Reitz, K. Binder, F. Bossle, F. Bracher, H. Bräunlich, E. Bretschneider, R. Brigelius-Flohé, K. Brinkmann, F. von Bruchhausen, A. Rüge, W. Christ, M. Cimbollek, R. Daniels, G. Dannhardt, H. Duchstein, S. Ebel, K. Eger, P. Eichhorn, U. Eiben, T. Erker, P. Felfe, A. Frahm, M. Frahm, V. Franke, K. Freundt, D. Geffken, U. Geis, E. Glusa, B. Göber, P. Gobina, W. Golder, M. Goppelt­Strübe, K. Götte, E. Gottstein, G. Greif, A. Grisk, M. Grosam, H. Gustmann, M. Gütschow, E. Hackenthal, A. Häfner, B. Haluszczynski, A. Harder, H. Häusler, D. Heber, M. Heidenreich, G. Heinemeyer, E. Heller, D. von Herrath, J. Hilfenhaus, H. Hoffmann, U. Hoffmann-Schollmayer, B. Hofmann, C. Holpert, U. Holzgrabe, U. Hübner-Steiner, M. Hug, E. Inkmann, A. Jördens, J. Jürgens, B. Kaiser, D. Kalbhen, H. Kemmler, P. Kisser, D. Kleinsorge, C. Klett, S. Klett, M. Klingmüller, H. Klöcking, A. Kramer, B. Krammer, M. Kreher, M. Krüger, M. Kuhn, D. Landsiedel-Maier, P. Lauven, J. Lehmann, M. Lehner, D. Leopoldt, A. Maurer, W. Meindl, K. Menges, P. Mes­singer, F. Meyer, W. Meyerhof, R. Morgenstern, U. Mühlhans, A. Müller, C. Müller, K. Müller, A. Mülsch, C. Nachtsheim, M. Neugebauer, W. Neupert, P. Nickel, P. Nuhn, B. Nürnberg, H. Oelschläger, J. Oertel, M. Oettel, R. Ott, T. Ott, T. Otzen, P. Pachaly, H. Pelzer, K. Petersen, R. Pick, M. Pickert, A. Pies, H. Priewer, O. Queckenberg, G. Radau, E. Reimann, J. Remien, M. Reuß, W. Reuß, J. Richter, P. Richter, K. Riecke, H. Rommelspacher, U. Rose, G. Roth, D. Rothley, G. Rücker, J. Schäfer, J. Schantl, H. Schlager, H. Schleinitz, W. Schlichter, M. Schmauß, H. Schmidhammer, G. Schmidt, T. Schmidt, H. Schmitt, J. Sehräder, T. Schulz, H. Schwilden, M. Serke, G. Skopp, G. Skorka, K. Smolinka, U. Speck, M. Spohn, R. Stahlmann, J. Stasch, C. Steffen, H. Stein, J. Steinmeyer, K. Stiefvater, G. Strippel, K. Surborg, U. Stürig, H. Szelényi, I. Szelényi, A. Täufel, R. Thieroff-Ekerdt, R. Troschütz, H. Ungeheuer, B. Unterhalt, E. Verspohl, S. Vogel, F. Volk, T. Vorwerk, J. Wallmann, H. Weber, M. Wenzel, M. Weyandt-Spangenberg, S. Wich, R. Wintersteiger, B. Wüst, and D. Youssef

Published
1999
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12. G

Author

Franz von Bruchhausen, Eberhard Hackenthal, Siegfried Ebel, Ulrike Holzgrabe, August Wilhelm Frahm, M. Albinus, G. Amschler, E. von Angerer, null Arras-Reiter, P. Barth, W. Barthel, K. Bauer, P. Bauer, I. Baumann, J. Beckmann, W. Beil, J. Reitz, K. Binder, F. Bossle, F. Bracher, H. Bräunlich, E. Bretschneider, R. Brigelius-Flohé, K. Brinkmann, F. von Bruchhausen, A. Rüge, W. Christ, M. Cimbollek, R. Daniels, G. Dannhardt, H. Duchstein, S. Ebel, K. Eger, P. Eichhorn, U. Eiben, T. Erker, P. Felfe, A. Frahm, M. Frahm, V. Franke, K. Freundt, D. Geffken, U. Geis, E. Glusa, B. Göber, P. Gobina, W. Golder, M. Goppelt­Strübe, K. Götte, E. Gottstein, G. Greif, A. Grisk, M. Grosam, H. Gustmann, M. Gütschow, E. Hackenthal, A. Häfner, B. Haluszczynski, A. Harder, H. Häusler, D. Heber, M. Heidenreich, G. Heinemeyer, E. Heller, D. von Herrath, J. Hilfenhaus, H. Hoffmann, U. Hoffmann-Schollmayer, B. Hofmann, C. Holpert, U. Holzgrabe, U. Hübner-Steiner, M. Hug, E. Inkmann, A. Jördens, J. Jürgens, B. Kaiser, D. Kalbhen, H. Kemmler, P. Kisser, D. Kleinsorge, C. Klett, S. Klett, M. Klingmüller, H. Klöcking, A. Kramer, B. Krammer, M. Kreher, M. Krüger, M. Kuhn, D. Landsiedel-Maier, P. Lauven, J. Lehmann, M. Lehner, D. Leopoldt, A. Maurer, W. Meindl, K. Menges, P. Mes­singer, F. Meyer, W. Meyerhof, R. Morgenstern, U. Mühlhans, A. Müller, C. Müller, K. Müller, A. Mülsch, C. Nachtsheim, M. Neugebauer, W. Neupert, P. Nickel, P. Nuhn, B. Nürnberg, H. Oelschläger, J. Oertel, M. Oettel, R. Ott, T. Ott, T. Otzen, P. Pachaly, H. Pelzer, K. Petersen, R. Pick, M. Pickert, A. Pies, H. Priewer, O. Queckenberg, G. Radau, E. Reimann, J. Remien, M. Reuß, W. Reuß, J. Richter, P. Richter, K. Riecke, H. Rommelspacher, U. Rose, G. Roth, D. Rothley, G. Rücker, J. Schäfer, J. Schantl, H. Schlager, H. Schleinitz, W. Schlichter, M. Schmauß, H. Schmidhammer, G. Schmidt, T. Schmidt, H. Schmitt, J. Sehräder, T. Schulz, H. Schwilden, M. Serke, G. Skopp, G. Skorka, K. Smolinka, U. Speck, M. Spohn, R. Stahlmann, J. Stasch, C. Steffen, H. Stein, J. Steinmeyer, K. Stiefvater, G. Strippel, K. Surborg, U. Stürig, H. Szelényi, I. Szelényi, A. Täufel, R. Thieroff-Ekerdt, R. Troschütz, H. Ungeheuer, B. Unterhalt, E. Verspohl, S. Vogel, F. Volk, T. Vorwerk, J. Wallmann, H. Weber, M. Wenzel, M. Weyandt-Spangenberg, S. Wich, R. Wintersteiger, B. Wüst, and D. Youssef

Published
1999
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13. F

Author

Franz von Bruchhausen, Eberhard Hackenthal, Siegfried Ebel, Ulrike Holzgrabe, August Wilhelm Frahm, M. Albinus, G. Amschler, E. von Angerer, null Arras-Reiter, P. Barth, W. Barthel, K. Bauer, P. Bauer, I. Baumann, J. Beckmann, W. Beil, J. Reitz, K. Binder, F. Bossle, F. Bracher, H. Bräunlich, E. Bretschneider, R. Brigelius-Flohé, K. Brinkmann, F. von Bruchhausen, A. Rüge, W. Christ, M. Cimbollek, R. Daniels, G. Dannhardt, H. Duchstein, S. Ebel, K. Eger, P. Eichhorn, U. Eiben, T. Erker, P. Felfe, A. Frahm, M. Frahm, V. Franke, K. Freundt, D. Geffken, U. Geis, E. Glusa, B. Göber, P. Gobina, W. Golder, M. Goppelt­Strübe, K. Götte, E. Gottstein, G. Greif, A. Grisk, M. Grosam, H. Gustmann, M. Gütschow, E. Hackenthal, A. Häfner, B. Haluszczynski, A. Harder, H. Häusler, D. Heber, M. Heidenreich, G. Heinemeyer, E. Heller, D. von Herrath, J. Hilfenhaus, H. Hoffmann, U. Hoffmann-Schollmayer, B. Hofmann, C. Holpert, U. Holzgrabe, U. Hübner-Steiner, M. Hug, E. Inkmann, A. Jördens, J. Jürgens, B. Kaiser, D. Kalbhen, H. Kemmler, P. Kisser, D. Kleinsorge, C. Klett, S. Klett, M. Klingmüller, H. Klöcking, A. Kramer, B. Krammer, M. Kreher, M. Krüger, M. Kuhn, D. Landsiedel-Maier, P. Lauven, J. Lehmann, M. Lehner, D. Leopoldt, A. Maurer, W. Meindl, K. Menges, P. Mes­singer, F. Meyer, W. Meyerhof, R. Morgenstern, U. Mühlhans, A. Müller, C. Müller, K. Müller, A. Mülsch, C. Nachtsheim, M. Neugebauer, W. Neupert, P. Nickel, P. Nuhn, B. Nürnberg, H. Oelschläger, J. Oertel, M. Oettel, R. Ott, T. Ott, T. Otzen, P. Pachaly, H. Pelzer, K. Petersen, R. Pick, M. Pickert, A. Pies, H. Priewer, O. Queckenberg, G. Radau, E. Reimann, J. Remien, M. Reuß, W. Reuß, J. Richter, P. Richter, K. Riecke, H. Rommelspacher, U. Rose, G. Roth, D. Rothley, G. Rücker, J. Schäfer, J. Schantl, H. Schlager, H. Schleinitz, W. Schlichter, M. Schmauß, H. Schmidhammer, G. Schmidt, T. Schmidt, H. Schmitt, J. Sehräder, T. Schulz, H. Schwilden, M. Serke, G. Skopp, G. Skorka, K. Smolinka, U. Speck, M. Spohn, R. Stahlmann, J. Stasch, C. Steffen, H. Stein, J. Steinmeyer, K. Stiefvater, G. Strippel, K. Surborg, U. Stürig, H. Szelényi, I. Szelényi, A. Täufel, R. Thieroff-Ekerdt, R. Troschütz, H. Ungeheuer, B. Unterhalt, E. Verspohl, S. Vogel, F. Volk, T. Vorwerk, J. Wallmann, H. Weber, M. Wenzel, M. Weyandt-Spangenberg, S. Wich, R. Wintersteiger, B. Wüst, and D. Youssef

Published
1999
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14. B

Author

Franz von Bruchhausen, Eberhard Hackenthal, Siegfried Ebel, Ulrike Holzgrabe, August Wilhelm Frahm, M. Albinus, G. Amschler, E. von Angerer, null Arras-Reiter, P. Barth, W. Barthel, K. Bauer, P. Bauer, I. Baumann, J. Beckmann, W. Beil, J. Reitz, K. Binder, F. Bossle, F. Bracher, H. Bräunlich, E. Bretschneider, R. Brigelius-Flohé, K. Brinkmann, F. von Bruchhausen, A. Rüge, W. Christ, M. Cimbollek, R. Daniels, G. Dannhardt, H. Duchstein, S. Ebel, K. Eger, P. Eichhorn, U. Eiben, T. Erker, P. Felfe, A. Frahm, M. Frahm, V. Franke, K. Freundt, D. Geffken, U. Geis, E. Glusa, B. Göber, P. Gobina, W. Golder, M. Goppelt­Strübe, K. Götte, E. Gottstein, G. Greif, A. Grisk, M. Grosam, H. Gustmann, M. Gütschow, E. Hackenthal, A. Häfner, B. Haluszczynski, A. Harder, H. Häusler, D. Heber, M. Heidenreich, G. Heinemeyer, E. Heller, D. von Herrath, J. Hilfenhaus, H. Hoffmann, U. Hoffmann-Schollmayer, B. Hofmann, C. Holpert, U. Holzgrabe, U. Hübner-Steiner, M. Hug, E. Inkmann, A. Jördens, J. Jürgens, B. Kaiser, D. Kalbhen, H. Kemmler, P. Kisser, D. Kleinsorge, C. Klett, S. Klett, M. Klingmüller, H. Klöcking, A. Kramer, B. Krammer, M. Kreher, M. Krüger, M. Kuhn, D. Landsiedel-Maier, P. Lauven, J. Lehmann, M. Lehner, D. Leopoldt, A. Maurer, W. Meindl, K. Menges, P. Mes­singer, F. Meyer, W. Meyerhof, R. Morgenstern, U. Mühlhans, A. Müller, C. Müller, K. Müller, A. Mülsch, C. Nachtsheim, M. Neugebauer, W. Neupert, P. Nickel, P. Nuhn, B. Nürnberg, H. Oelschläger, J. Oertel, M. Oettel, R. Ott, T. Ott, T. Otzen, P. Pachaly, H. Pelzer, K. Petersen, R. Pick, M. Pickert, A. Pies, H. Priewer, O. Queckenberg, G. Radau, E. Reimann, J. Remien, M. Reuß, W. Reuß, J. Richter, P. Richter, K. Riecke, H. Rommelspacher, U. Rose, G. Roth, D. Rothley, G. Rücker, J. Schäfer, J. Schantl, H. Schlager, H. Schleinitz, W. Schlichter, M. Schmauß, H. Schmidhammer, G. Schmidt, T. Schmidt, H. Schmitt, J. Sehräder, T. Schulz, H. Schwilden, M. Serke, G. Skopp, G. Skorka, K. Smolinka, U. Speck, M. Spohn, R. Stahlmann, J. Stasch, C. Steffen, H. Stein, J. Steinmeyer, K. Stiefvater, G. Strippel, K. Surborg, U. Stürig, H. Szelényi, I. Szelényi, A. Täufel, R. Thieroff-Ekerdt, R. Troschütz, H. Ungeheuer, B. Unterhalt, E. Verspohl, S. Vogel, F. Volk, T. Vorwerk, J. Wallmann, H. Weber, M. Wenzel, M. Weyandt-Spangenberg, S. Wich, R. Wintersteiger, B. Wüst, and D. Youssef

Published
1999
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15. K

Author

Franz von Bruchhausen, Eberhard Hackenthal, Siegfried Ebel, Ulrike Holzgrabe, August Wilhelm Frahm, M. Albinus, G. Amschler, E. von Angerer, null Arras-Reiter, P. Barth, W. Barthel, K. Bauer, P. Bauer, I. Baumann, J. Beckmann, W. Beil, J. Reitz, K. Binder, F. Bossle, F. Bracher, H. Bräunlich, E. Bretschneider, R. Brigelius-Flohé, K. Brinkmann, F. von Bruchhausen, A. Rüge, W. Christ, M. Cimbollek, R. Daniels, G. Dannhardt, H. Duchstein, S. Ebel, K. Eger, P. Eichhorn, U. Eiben, T. Erker, P. Felfe, A. Frahm, M. Frahm, V. Franke, K. Freundt, D. Geffken, U. Geis, E. Glusa, B. Göber, P. Gobina, W. Golder, M. Goppelt­Strübe, K. Götte, E. Gottstein, G. Greif, A. Grisk, M. Grosam, H. Gustmann, M. Gütschow, E. Hackenthal, A. Häfner, B. Haluszczynski, A. Harder, H. Häusler, D. Heber, M. Heidenreich, G. Heinemeyer, E. Heller, D. von Herrath, J. Hilfenhaus, H. Hoffmann, U. Hoffmann-Schollmayer, B. Hofmann, C. Holpert, U. Holzgrabe, U. Hübner-Steiner, M. Hug, E. Inkmann, A. Jördens, J. Jürgens, B. Kaiser, D. Kalbhen, H. Kemmler, P. Kisser, D. Kleinsorge, C. Klett, S. Klett, M. Klingmüller, H. Klöcking, A. Kramer, B. Krammer, M. Kreher, M. Krüger, M. Kuhn, D. Landsiedel-Maier, P. Lauven, J. Lehmann, M. Lehner, D. Leopoldt, A. Maurer, W. Meindl, K. Menges, P. Mes­singer, F. Meyer, W. Meyerhof, R. Morgenstern, U. Mühlhans, A. Müller, C. Müller, K. Müller, A. Mülsch, C. Nachtsheim, M. Neugebauer, W. Neupert, P. Nickel, P. Nuhn, B. Nürnberg, H. Oelschläger, J. Oertel, M. Oettel, R. Ott, T. Ott, T. Otzen, P. Pachaly, H. Pelzer, K. Petersen, R. Pick, M. Pickert, A. Pies, H. Priewer, O. Queckenberg, G. Radau, E. Reimann, J. Remien, M. Reuß, W. Reuß, J. Richter, P. Richter, K. Riecke, H. Rommelspacher, U. Rose, G. Roth, D. Rothley, G. Rücker, J. Schäfer, J. Schantl, H. Schlager, H. Schleinitz, W. Schlichter, M. Schmauß, H. Schmidhammer, G. Schmidt, T. Schmidt, H. Schmitt, J. Sehräder, T. Schulz, H. Schwilden, M. Serke, G. Skopp, G. Skorka, K. Smolinka, U. Speck, M. Spohn, R. Stahlmann, J. Stasch, C. Steffen, H. Stein, J. Steinmeyer, K. Stiefvater, G. Strippel, K. Surborg, U. Stürig, H. Szelényi, I. Szelényi, A. Täufel, R. Thieroff-Ekerdt, R. Troschütz, H. Ungeheuer, B. Unterhalt, E. Verspohl, S. Vogel, F. Volk, T. Vorwerk, J. Wallmann, H. Weber, M. Wenzel, M. Weyandt-Spangenberg, S. Wich, R. Wintersteiger, B. Wüst, and D. Youssef

Published
1999
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16. The glycine site on the NMDA receptor: structure-activity relationships and possible therapeutic applications

Author

G, Dannhardt and B K, Kohl

Subjects
Cerebrovascular Disorders, Structure-Activity Relationship, Binding Sites, Epilepsy, Neuroprotective Agents, Alzheimer Disease, Glycine, Schizophrenia, Animals, Humans, Neurodegenerative Diseases, Parkinson Disease, Receptors, N-Methyl-D-Aspartate
Abstract

L-glutamate is the most important fast excitatory neurotransmitter in the mammalian central nervous system. Glutamate receptors are classified into two main categories: ionotropic and metabotropic. The N-methyl-D-aspartate (NMDA) receptor, which is associated with an ion channel, seems to play an important role in glutamate excitotoxicity, a process thought to be involved in a number of neurodegenerative disorders such as focal cerebral ischaemia (stroke), Parkinsonís, Huntingtonís, Alzheimerís disease, schizophrenia and epilepsy. The unique glycine site on the NMDA receptor, discovered by Johnson and Ascher in 1987, represents an interesting target for the development of neuroprotective compounds. Glycine antagonists may offer advantages over other NMDA antagonists in terms of their side-effect profile, especially in the long-term treatment of chronical neurodegenerative disorders but also in the treatment of serious medical emergencies with a significant morbidity and mortality like status epilepticus or stroke. So far it is not clear whether NMDA receptor antagonists including glycine antagonists would be suitable for chronic administration because of their effects on cognition, learning and motor function. High-affinity, in vivo potent, glycine antagonists of great structural diversity (i. e. pyrido[2,3-b]pyrazine-N-oxides, indole-2-carboxylates, 4-substituted-3-phenylquinoline-2(1H)-ones and alkyl-substituted 1,4-dihydro-quinoxaline-2,3-diones) are now available and their suitability for long-term treatment of chronical neurodegenerative disorders has to be investigated in clinical trials.

Published
1998

17. [2-Aryl-pyrrolo[2,1-b]benzothiazoles as a selective or dual inhibitors of cyclo-oxygenases and 5-lipoxygenases. 21. Non-steroidal anti-inflammatory agents]

Author

G, Dannhardt, M, Kreher, U, Nowe, and S, Schmitt

Subjects
Structure-Activity Relationship, Thiazoles, Magnetic Resonance Spectroscopy, Neutrophils, Anti-Inflammatory Agents, Non-Steroidal, Humans, Cyclooxygenase Inhibitors, Lipoxygenase Inhibitors, In Vitro Techniques
Abstract

A series of 2-aryl-pyrrolobenzothiazoles with additional functional groups was synthesized and characterized. Mainly ring opening and less substitution of the pyrrole moiety was observed reacting the heterocyclic system with diazoethyl acetate. In general all compounds inhibit 5-lipoxygenase more effectively than cyclooxygenase but one of them is a well balanced dual inhibitor. A structure-activity relationship and the enzyme selectivity are discussed.

Published
1997

18. Non-steroidal anti-inflammatory agents, Part 24. Pyrrolidino enaminones as models to mimic arachidonic acid

Author

G, Dannhardt, A, Bauer, and U, Nowe

Subjects
Blood Platelets, Structure-Activity Relationship, Arachidonic Acid, Neutrophils, Anti-Inflammatory Agents, Non-Steroidal, Animals, Cattle, Cyclooxygenase Inhibitors, In Vitro Techniques, Pyrrolidinones
Abstract

The pyrrolidino enaminones, with the carboxylic acid chain fixed at the nitrogen, inhibit cyclooxygenase more potently or selectively than 5-lipoxygenase. According to the structure-activity relationships discussed the potency depends significantly on the chain length of the carboxylic acid, the substitution pattern of the heterocyclic moiety and of the phenyl group. Compound 4c is the most efficient inhibitor of cyclooxygenase. For the binding profile the unfolded conformation of arachidonic acid and the energy-minimized conformations of flurbiprofen, diclofenac, ML 3000, and lead compound 4a were compared. In addition to known structural features, similar distances of the carboxylic acid function and the phenyl residue were found as hypothesized to explain the interaction with the active sites of the enzyme. The inhibition of cyclooxygenase was determined in a bovine thrombocyte intact cell assay and that of 5-lipoxygenase using intact bovine PMNLs.

Published
1997

19. Pyrrolidino enaminones structural related to gyrase inhibitors: synthesis, cyclization and pharmacological activity

Author

G, Dannhardt and A, Bauer

Subjects
Structure-Activity Relationship, Pyrrolidines, Bacteria, Cyclization, Molecular Conformation, Topoisomerase II Inhibitors, Enzyme Inhibitors, Crystallography, X-Ray, Anti-Bacterial Agents
Abstract

The synthesis and stereochemical characteristics of pyrrolidino enaminones with structural analogy to quinolone antibacterial agents are reported. Retro-aldol reaction of the esters 7 is observed under all conditions of hydrolysis, the enzyme catalyzed reaction also does not yield the corresponding acids. In contrast to clinically used quinolones exemplary tests with monocyclic esters of type 7 and the tricyclic derivative 10 indicate low or no antibacterial activity. Additionally to the lack of the carboxylic acid function the enaminones 7 differ from quinolones in stereochemical demands and the electronic situation of the phenyl substituents of 10, respectively possibly preventing the formation of a co-operative tetrametric system between compounds and DNA bases.

Published
1996

20. Non-steroidal anti-inflammatory agents, Part 20. Method for testing non-steroidal anti-inflammatories: the modified hen's egg chorioallantoic membrane test (HET-CAM test) compared to other procedures

Author

G, Dannhardt, M, Kreher, U, Nowe, and A, Pies

Subjects
Diffusion, Time Factors, Dose-Response Relationship, Drug, Molecular Structure, Eggs, Anti-Inflammatory Agents, Non-Steroidal, Toxicity Tests, Animals, Chorion, Chickens
Abstract

The delay of onset of irritation phenomena at the chorioallantoic membrane of incubated hen's eggs, a parameter for anti-inflammatory activity, was determined for the pharmaceutical substances diclofenac, flufenamic acid, ibuprofen, indomethacin, ketoprofen, piroxicam, phenylbutazone, salicylic acid, and sodium salicylate. Alongside questions relating to the dose-effect ratio, metabolisation, recovery, and diffusion of the substances to their site of action were investigated. The reproducibility of the procedure and its selectivity with regard to substances with a different mechanism of action is proven. The method allows classification of the substances according to their anti-inflammatory potency. However, correlation with the results of enzyme inhibition or in vivo results is only possible to a limited extent.

Published
1996

21. Pharmacological profile of a new pyrrolizine derivative inhibiting the enzymes cyclo-oxygenase and 5-lipoxygenase

Author

S, Laufer, S, Tries, J, Augustin, and G, Dannhardt

Subjects
Male, Mice, Inbred ICR, Arachidonic Acid, Platelet Aggregation, Bronchoconstriction, Guinea Pigs, Acetates, In Vitro Techniques, Carrageenan, Arthritis, Experimental, Rats, Rats, Sprague-Dawley, Mice, Yeast, Dried, Benzoquinones, Animals, Edema, Cyclooxygenase Inhibitors, Female, Pyrroles, Lipoxygenase Inhibitors, Rabbits, Blood Coagulation, Platelet Aggregation Inhibitors, Pain Measurement
Abstract

2,2-Dimethyl-6-(4-chlorophenyl)-7-phenyl, 2,3-dihydro-1H-pyrrolizine-5-yl)-acetic acid (ML 3000) is a dual inhibitor of the enzymes cyclo-oxygenase and 5-lipoxygenase in bovine and human thrombocytes and granulocytes. In animal experiments the compound has antiphlogistic, analgesic, antipyretic, antiasthmatic and antiaggregative activity at a dosage that causes no gastrointestinal damage.

Published
1994

23. Hypertensive effects and structure-activity relationships of 5-omega-aminoalkyl isoxazoles

Author

G, Dannhardt, P, Dominiak, and S, Laufer

Subjects
Decerebrate State, Male, Rats, Sprague-Dawley, Structure-Activity Relationship, Heart Rate, Animals, Blood Pressure, Isoxazoles, Stimulation, Chemical, Rats
Abstract

Structure-activity and dose-response relationships of a series of novel 5-omega aminoalkyl and 5-omega-amino-heteroalkyl isoxazoles on blood pressure and heart rate of Sprague-Dawley rats have been investigated. To differentiate between peripheral and central cardiovascular actions of those compounds a pithed rat and anaesthetized rat preparation was used. Most of the compounds investigated exhibit potent hypertensive actions. The hypertensive effects of the tested compounds is depending on the amphiphilic character of the isoxazoles represented by a basic moiety in a definite distance to the phenyl substituents. To achieve high pharmacological activity a fully flexible side chain is requested, too. Possible mechanisms of action are discussed.

Published
1993

24. J

Author

F. von Bruchhausen, G. Dannhardt, S. Ebel, A. W. Frahm, E. Hackenthal, R. Hänsel, U. Holzgrabe, K. Keller, E. Nürnberg, H. Rimpler, G. Schneider, P. Surmann, H. U. Wolf, G. Wurm, R. D. Aye, G. Bader, I. Bauer, R. Bauer, H. Becker, G. Beyer, W. Blaschek, N. Brand, U. Braun-Sprakties, R. Brenneisen, R. Broese, A. Burger, J. Burghart, N. Chaurasia, W. Cholcha, U. Eilert, D. Ennet, W. Ferstl, E. Fiegert, F. Gaedcke, B. Gehrmann, K. Gomaa, P. Gorecki, M. W. Grubert, G. Harnischfeger, H. J. Helmlin, G. Henkler, A. Hensel, G. Heubl, A. Hiermann, K. Hiller, K. Hoffmann-Bohm, B. Hohmann, W. Holz, J. Hölzl, K. H. Horz, O. Isaac, C. Jerga, W. Juretzek, T. Kartnig, H. P. Koch, H. Koehler, L. Kraus, W. Kreis, E. Leng-Peschlow, R. Liersch, U. Lindequist, E. Mechler, B. Meier, M. Meier-Liebi, H. G. Menßen, I. Merfort, H. Miething, S. Moeck, S. Mundt, K. Münzing-Vasirian, S. Noster, N. Ohem, D. Paper, J. Reichling, W. Schilz, H. Schleinitz, E. Schneider, E. Scholz, T. Schöpke, V. Schulz, H. Schütt, H. Schwarze, S. Schweins, B. Schwell, R. Seitz, U. Sonnenborn, E. Spieß, V. Ssymank, K. Staesche, E. Stahl-Biskup, H. Stuppner, E. Teuscher, M. Veit, A. Wiebrecht, M. Wink, U. Wissinger-Gräfenhahn, R. Wohlfart, and B. Zepernick

Published
1993
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25. I

Author

F. von Bruchhausen, G. Dannhardt, S. Ebel, A. W. Frahm, E. Hackenthal, R. Hänsel, U. Holzgrabe, K. Keller, E. Nürnberg, H. Rimpler, G. Schneider, P. Surmann, H. U. Wolf, G. Wurm, R. D. Aye, G. Bader, I. Bauer, R. Bauer, H. Becker, G. Beyer, W. Blaschek, N. Brand, U. Braun-Sprakties, R. Brenneisen, R. Broese, A. Burger, J. Burghart, N. Chaurasia, W. Cholcha, U. Eilert, D. Ennet, W. Ferstl, E. Fiegert, F. Gaedcke, B. Gehrmann, K. Gomaa, P. Gorecki, M. W. Grubert, G. Harnischfeger, H. J. Helmlin, G. Henkler, A. Hensel, G. Heubl, A. Hiermann, K. Hiller, K. Hoffmann-Bohm, B. Hohmann, W. Holz, J. Hölzl, K. H. Horz, O. Isaac, C. Jerga, W. Juretzek, T. Kartnig, H. P. Koch, H. Koehler, L. Kraus, W. Kreis, E. Leng-Peschlow, R. Liersch, U. Lindequist, E. Mechler, B. Meier, M. Meier-Liebi, H. G. Menßen, I. Merfort, H. Miething, S. Moeck, S. Mundt, K. Münzing-Vasirian, S. Noster, N. Ohem, D. Paper, J. Reichling, W. Schilz, H. Schleinitz, E. Schneider, E. Scholz, T. Schöpke, V. Schulz, H. Schütt, H. Schwarze, S. Schweins, B. Schwell, R. Seitz, U. Sonnenborn, E. Spieß, V. Ssymank, K. Staesche, E. Stahl-Biskup, H. Stuppner, E. Teuscher, M. Veit, A. Wiebrecht, M. Wink, U. Wissinger-Gräfenhahn, R. Wohlfart, and B. Zepernick

Published
1993
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26. Labetalol

Author

F. von Bruchhausen, S. Ebel, E. Hackenthal, G. Dannhardt, A. W. Frahm, U. Holzgrabe, K. Keller, E. Nürnberg, H. Rimpler, G. Schneider, P. Surmann, H. U. Wolf, and G. Wurm

Published
1993
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27. Famotidin

Author

F. von Bruchhausen, S. Ebel, E. Hackenthal, G. Dannhardt, A. W. Frahm, U. Holzgrabe, K. Keller, E. Nürnberg, H. Rimpler, G. Schneider, P. Surmann, H. U. Wolf, and G. Wurm

Published
1993
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28. Econazol

Author

F. von Bruchhausen, S. Ebel, E. Hackenthal, G. Dannhardt, A. W. Frahm, U. Holzgrabe, K. Keller, E. Nürnberg, H. Rimpler, G. Schneider, P. Surmann, H. U. Wolf, and G. Wurm

Published
1993
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29. O

Author

F. von Bruchhausen, G. Dannhardt, S. Ebel, A. W. Frahm, E. Hackenthal, R. Hänsel, U. Holzgrabe, K. Keller, E. Nürnberg, H. Rimpler, G. Schneider, P. Surmann, H. U. Wolf, G. Wurm, R. D. Aye, G. Bader, I. Bauer, R. Bauer, H. Becker, G. Beyer, W. Blaschek, N. Brand, U. Braun-Sprakties, R. Brenneisen, R. Broese, A. Burger, J. Burghart, N. Chaurasia, W. Cholcha, U. Eilert, D. Ennet, W. Ferstl, E. Fiegert, F. Gaedcke, B. Gehrmann, K. Gomaa, P. Gorecki, M. W. Grubert, G. Harnischfeger, H. J. Helmlin, G. Henkler, A. Hensel, G. Heubl, A. Hiermann, K. Hiller, K. Hoffmann-Bohm, B. Hohmann, W. Holz, J. Hölzl, K. H. Horz, O. Isaac, C. Jerga, W. Juretzek, T. Kartnig, H. P. Koch, H. Koehler, L. Kraus, W. Kreis, E. Leng-Peschlow, R. Liersch, U. Lindequist, E. Mechler, B. Meier, M. Meier-Liebi, H. G. Menßen, I. Merfort, H. Miething, S. Moeck, S. Mundt, K. Münzing-Vasirian, S. Noster, N. Ohem, D. Paper, J. Reichling, W. Schilz, H. Schleinitz, E. Schneider, E. Scholz, T. Schöpke, V. Schulz, H. Schütt, H. Schwarze, S. Schweins, B. Schwell, R. Seitz, U. Sonnenborn, E. Spieß, V. Ssymank, K. Staesche, E. Stahl-Biskup, H. Stuppner, E. Teuscher, M. Veit, A. Wiebrecht, M. Wink, U. Wissinger-Gräfenhahn, R. Wohlfart, and B. Zepernick

Published
1993
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30. H

Author

F. von Bruchhausen, G. Dannhardt, S. Ebel, A. W. Frahm, E. Hackenthal, R. Hänsel, U. Holzgrabe, K. Keller, E. Nürnberg, H. Rimpler, G. Schneider, P. Surmann, H. U. Wolf, G. Wurm, R. D. Aye, G. Bader, I. Bauer, R. Bauer, H. Becker, G. Beyer, W. Blaschek, N. Brand, U. Braun-Sprakties, R. Brenneisen, R. Broese, A. Burger, J. Burghart, N. Chaurasia, W. Cholcha, U. Eilert, D. Ennet, W. Ferstl, E. Fiegert, F. Gaedcke, B. Gehrmann, K. Gomaa, P. Gorecki, M. W. Grubert, G. Harnischfeger, H. J. Helmlin, G. Henkler, A. Hensel, G. Heubl, A. Hiermann, K. Hiller, K. Hoffmann-Bohm, B. Hohmann, W. Holz, J. Hölzl, K. H. Horz, O. Isaac, C. Jerga, W. Juretzek, T. Kartnig, H. P. Koch, H. Koehler, L. Kraus, W. Kreis, E. Leng-Peschlow, R. Liersch, U. Lindequist, E. Mechler, B. Meier, M. Meier-Liebi, H. G. Menßen, I. Merfort, H. Miething, S. Moeck, S. Mundt, K. Münzing-Vasirian, S. Noster, N. Ohem, D. Paper, J. Reichling, W. Schilz, H. Schleinitz, E. Schneider, E. Scholz, T. Schöpke, V. Schulz, H. Schütt, H. Schwarze, S. Schweins, B. Schwell, R. Seitz, U. Sonnenborn, E. Spieß, V. Ssymank, K. Staesche, E. Stahl-Biskup, H. Stuppner, E. Teuscher, M. Veit, A. Wiebrecht, M. Wink, U. Wissinger-Gräfenhahn, R. Wohlfart, and B. Zepernick

Published
1993
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31. M

Author

F. von Bruchhausen, G. Dannhardt, S. Ebel, A. W. Frahm, E. Hackenthal, R. Hänsel, U. Holzgrabe, K. Keller, E. Nürnberg, H. Rimpler, G. Schneider, P. Surmann, H. U. Wolf, G. Wurm, R. D. Aye, G. Bader, I. Bauer, R. Bauer, H. Becker, G. Beyer, W. Blaschek, N. Brand, U. Braun-Sprakties, R. Brenneisen, R. Broese, A. Burger, J. Burghart, N. Chaurasia, W. Cholcha, U. Eilert, D. Ennet, W. Ferstl, E. Fiegert, F. Gaedcke, B. Gehrmann, K. Gomaa, P. Gorecki, M. W. Grubert, G. Harnischfeger, H. J. Helmlin, G. Henkler, A. Hensel, G. Heubl, A. Hiermann, K. Hiller, K. Hoffmann-Bohm, B. Hohmann, W. Holz, J. Hölzl, K. H. Horz, O. Isaac, C. Jerga, W. Juretzek, T. Kartnig, H. P. Koch, H. Koehler, L. Kraus, W. Kreis, E. Leng-Peschlow, R. Liersch, U. Lindequist, E. Mechler, B. Meier, M. Meier-Liebi, H. G. Menßen, I. Merfort, H. Miething, S. Moeck, S. Mundt, K. Münzing-Vasirian, S. Noster, N. Ohem, D. Paper, J. Reichling, W. Schilz, H. Schleinitz, E. Schneider, E. Scholz, T. Schöpke, V. Schulz, H. Schütt, H. Schwarze, S. Schweins, B. Schwell, R. Seitz, U. Sonnenborn, E. Spieß, V. Ssymank, K. Staesche, E. Stahl-Biskup, H. Stuppner, E. Teuscher, M. Veit, A. Wiebrecht, M. Wink, U. Wissinger-Gräfenhahn, R. Wohlfart, and B. Zepernick

Published
1993
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32. N

Author

F. von Bruchhausen, G. Dannhardt, S. Ebel, A. W. Frahm, E. Hackenthal, R. Hänsel, U. Holzgrabe, K. Keller, E. Nürnberg, H. Rimpler, G. Schneider, P. Surmann, H. U. Wolf, G. Wurm, R. D. Aye, G. Bader, I. Bauer, R. Bauer, H. Becker, G. Beyer, W. Blaschek, N. Brand, U. Braun-Sprakties, R. Brenneisen, R. Broese, A. Burger, J. Burghart, N. Chaurasia, W. Cholcha, U. Eilert, D. Ennet, W. Ferstl, E. Fiegert, F. Gaedcke, B. Gehrmann, K. Gomaa, P. Gorecki, M. W. Grubert, G. Harnischfeger, H. J. Helmlin, G. Henkler, A. Hensel, G. Heubl, A. Hiermann, K. Hiller, K. Hoffmann-Bohm, B. Hohmann, W. Holz, J. Hölzl, K. H. Horz, O. Isaac, C. Jerga, W. Juretzek, T. Kartnig, H. P. Koch, H. Koehler, L. Kraus, W. Kreis, E. Leng-Peschlow, R. Liersch, U. Lindequist, E. Mechler, B. Meier, M. Meier-Liebi, H. G. Menßen, I. Merfort, H. Miething, S. Moeck, S. Mundt, K. Münzing-Vasirian, S. Noster, N. Ohem, D. Paper, J. Reichling, W. Schilz, H. Schleinitz, E. Schneider, E. Scholz, T. Schöpke, V. Schulz, H. Schütt, H. Schwarze, S. Schweins, B. Schwell, R. Seitz, U. Sonnenborn, E. Spieß, V. Ssymank, K. Staesche, E. Stahl-Biskup, H. Stuppner, E. Teuscher, M. Veit, A. Wiebrecht, M. Wink, U. Wissinger-Gräfenhahn, R. Wohlfart, and B. Zepernick

Published
1993
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33. K

Author

F. von Bruchhausen, G. Dannhardt, S. Ebel, A. W. Frahm, E. Hackenthal, R. Hänsel, U. Holzgrabe, K. Keller, E. Nürnberg, H. Rimpler, G. Schneider, P. Surmann, H. U. Wolf, G. Wurm, R. D. Aye, G. Bader, I. Bauer, R. Bauer, H. Becker, G. Beyer, W. Blaschek, N. Brand, U. Braun-Sprakties, R. Brenneisen, R. Broese, A. Burger, J. Burghart, N. Chaurasia, W. Cholcha, U. Eilert, D. Ennet, W. Ferstl, E. Fiegert, F. Gaedcke, B. Gehrmann, K. Gomaa, P. Gorecki, M. W. Grubert, G. Harnischfeger, H. J. Helmlin, G. Henkler, A. Hensel, G. Heubl, A. Hiermann, K. Hiller, K. Hoffmann-Bohm, B. Hohmann, W. Holz, J. Hölzl, K. H. Horz, O. Isaac, C. Jerga, W. Juretzek, T. Kartnig, H. P. Koch, H. Koehler, L. Kraus, W. Kreis, E. Leng-Peschlow, R. Liersch, U. Lindequist, E. Mechler, B. Meier, M. Meier-Liebi, H. G. Menßen, I. Merfort, H. Miething, S. Moeck, S. Mundt, K. Münzing-Vasirian, S. Noster, N. Ohem, D. Paper, J. Reichling, W. Schilz, H. Schleinitz, E. Schneider, E. Scholz, T. Schöpke, V. Schulz, H. Schütt, H. Schwarze, S. Schweins, B. Schwell, R. Seitz, U. Sonnenborn, E. Spieß, V. Ssymank, K. Staesche, E. Stahl-Biskup, H. Stuppner, E. Teuscher, M. Veit, A. Wiebrecht, M. Wink, U. Wissinger-Gräfenhahn, R. Wohlfart, and B. Zepernick

Published
1993
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34. Gabexat

Author

F. von Bruchhausen, S. Ebel, E. Hackenthal, G. Dannhardt, A. W. Frahm, U. Holzgrabe, K. Keller, E. Nürnberg, H. Rimpler, G. Schneider, P. Surmann, H. U. Wolf, and G. Wurm

Published
1993
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35. [Hypertensive action of 5-(beta-aminoethyl)aminoisoxazoles: synthesis and screening of isoxazolopyrazines and isoxazolodiazepines]

Author

G, Dannhardt, P, Dominiak, and S, Laufer

Subjects
Decerebrate State, Male, Structure-Activity Relationship, Heart Rate, Pyrazines, Animals, Blood Pressure, Rats, Inbred Strains, Azepines, Isoxazoles, Rats
Abstract

The 5-aminoisoxazole 1 is converted via the 4-nitro derivative to the 4,5-diamino compound 4, which cyclises with glyoxal to yield the isoxazolo[4,5-b)pyrazine 5. Decomposition of the isoxazole moiety is always observed in experiments to hydrogenate partially the pyrazine ring and to phenylate the N-atom, respectively. Therefore, the corresponding tetrahydro derivative 6 is prepared from 4 and 1,2-ethandiol ditosylate. Starting with benzohydroxamic acid chloride and a cyanoacetic acid amide the tetrahydro isoxazolo[5,4-e]1,4-diazepinone-4 18 is synthesized. All new compounds are characterized by their spectroscopic data, the reaction mechanisms are discussed. Using the model of the pithed and the anaesthetized rat, resp., the pyrazino- and diazepino-isoxazoles (compounds 5, 6, 13, 18) have less or no hypertensive activity as compared to the corresponding derivatives with fully flexible side chains.

Published
1991

36. [Hypertensive acting 5-(beta-aminoethyl)aminoisoxazoles: synthesis and screening of derivatives with with partially rigid C-5 side chains and omega-position heterocyclics]

Author

G, Dannhardt, P, Dominiak, and S, Laufer

Subjects
Decerebrate State, Male, Structure-Activity Relationship, Hemodynamics, Animals, Anesthesia, Rats, Inbred Strains, Isoxazoles, Diamines, Antihypertensive Agents, Rats
Abstract

Isoxazoles with a 1,2-diaminoethane side chain at C-5 are synthesized by nucleophilic substitution of 5-chloro derivatives. Using piperazine, imidazolidine and 1,2-diaminocyclohexane, resp., isoxazoles with partially rigid chains at C-5 are formed. The same procedure succeeds in the synthesis of isoxazoles having a heterocycle at the omega-position of the side chain. The hypertensive activity of all new compounds is shown for the pithed and the anaesthetized rat, resp. According to structure activity relationships the hypertensive activity of compounds 7 and 8, resp., is mainly determined by the heterocycle at the omega-position (piperazine greater than piperidine approximately pyrrolidine greater than morpholine). Derivatives 2-5 with partially rigid 5-(beta-aminoethyl)amino side chains show less hypertensive activity than the corresponding compounds without restrictions.

Published
1990

38. [Antimycobacterial acting 2-hydroxyquinolizin-4-ones]

Author

G, Dannhardt, T, Kappe, W, Meindl, and B, Schober

Subjects
Chemistry, Structure-Activity Relationship, Chemical Phenomena, Microbial Sensitivity Tests, Mycobacterium tuberculosis, Quinolizines
Abstract

Reaction of ethyl 2-pyridyl acetates and activated malonates (magic malonates) leads to 1-ethoxycarbonyl-2-hydroxy-quinolizin-4-ones, which yield the corresponding C-1 unsubstituted derivatives by hydrolysis and decarboxylation. These compounds are catalytically hydrogenated to afford the corresponding tetrahydro derivatives. Significant inhibitory effects on mycobacterium tuberculosis H 37 Ra are shown, a structure-activity relationship is discussed.

Published
1990

40. Preface

Author

G. Dannhardt

Subjects
Pharmacology, Drug Discovery, Organic Chemistry, Molecular Medicine, Biochemistry
Published
2000
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41. Alkaloids ofLolium temulentum:Isolation, Identification and Pharmacological Activity1

Author

G. Dannhardt and L. Steindl

Subjects
Pharmacology, Lolium temulentum, biology, Stereochemistry, Alkaloid, Organic Chemistry, Pharmaceutical Science, Biological activity, Bungarotoxin, biology.organism_classification, Analytical Chemistry, Caryopsis, Complementary and alternative medicine, Drug Discovery, Prazosin, medicine, Molecular Medicine, Flunitrazepam, Binding site, medicine.drug
Abstract

Analysis of the overground part of LOLIUM TEMULENTUM L. led to the isolation of two main alkaloids: loline ( B) and perloline ( D). Loline and two minor alkaloids ( A, C) are strictly localized in the caryopses, whereas perloline is found mainly in the stems. In tests for CNS activity loline · 2 HCl was uneffective in displacing prazosin, serotonine, QNB, bungarotoxin and flunitrazepam from binding sites of calf brain.

Published
1985
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