Search Results - "Carsten Schmeck"

Small molecules and their impact in drug discovery: A perspective on the occasion of the 125th anniversary of the Bayer Chemical Research Laboratory by Beck, Hartmut, Härter, Michael, Haß, Bastian, Schmeck, Carsten, Baerfacker, Lars

“…•Bayer celebrates its long history in small molecule drug discovery.•Small molecule drugs have always played a major role in the progress of medicine.•Small…”
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Stereoselective Mukaiyama-Michael/Michael/Aldol Domino Cyclization as the Key Step in the Synthesis of Pentasubstituted Arenes: An Efficient Access to Highly Active Inhibitors of Cholesteryl Ester Transfer Protein (CETP) by Paulsen, Holger, Antons, Stefan, Brandes, Arndt, Lögers, Michael, Müller, Stephan Nicholas, Naab, Paul, Schmeck, Carsten, Schneider, Stephan, Stoltefuß, Jürgen

“…Seemingly heartbreaking for a stereochemist, the one‐step selective construction of a stereopentad and its prompt destruction by aromatization has been proven…”
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Synthesis of Optically Active 4-Substituted 2-Aminobutyrolactones and Homoserines by Combined Aldol/Photocyclization Reactions of Chromium Aminocarbene Complexes by Schmeck, Carsten, Hegedus, Louis S

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Pharmacological inhibition of Vanin-1 is not protective in models of acute and chronic kidney disease by Unterschemmann, Kerstin, Ehrmann, Alexander, Herzig, Ina, Andreevski, Anna-Lena, Lustig, Klemens, Schmeck, Carsten, Eitner, Frank, Grundmann, Manuel

“…Oxidative stress is a key concept in basic, translational, and clinical research to understand the pathophysiology of various disorders, including…”
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Cardiac output improvement by pecavaptan: a novel dual‐acting vasopressin V1a/V2 receptor antagonist in experimental heart failure by Mondritzki, Thomas, Mai, Thuy Anh, Vogel, Julia, Pook, Elisabeth, Wasnaire, Pierre, Schmeck, Carsten, Hüser, Jörg, Dinh, Wilfried, Truebel, Hubert, Kolkhof, Peter

“…Aims Arginine vasopressin (AVP) mediates deleterious effects via vascular V1a and renal V2 receptors in heart failure (HF). Despite positive short‐term…”
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Pharmacological Inhibition of Vanin 1 Is Not Protective in Models of Acute and Chronic Kidney Disease: PO2372 by Unterschemmann, Kerstin D., Ehrmann, Alexander, Herzig, Ina D., Andreevski, Anna Lena, Schmeck, Carsten, Eitner, Frank, Grundmann, Manuel

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Fluorine-Substitution in Cholesteryl Ester Transfer Protein Inhibitors (CETPInhibitors) – Biology, Chemistry, SAR, and Properties by Holger Paulsena, Siegfried Zaiss, Delf Schmidt, Hilmar Bischoff, Klaus-Dieter Bremm, Paul Naab, Michael Lögers, Stephan N. Wirtz, Jürgen Stoltefuss, Gunter Schmidt, Arndt Brandes, Carsten Schmeck, Stefan Antons

“…The inhibition of the cholesteryl ester transfer protein (CETP) provides a method for the elevation of the high density lipoprotein cholesterol (HDL-C) level,…”
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Vascular Protection and Decongestion Without Renin–Angiotensin–Aldosterone System Stimulation Mediated by a Novel Dual-Acting Vasopressin V1a/V2 Receptor Antagonist by Kolkhof, Peter, Pook, Elisabeth, Pavkovic, Mira, Kretschmer, Axel, Buchmüller, Anja, Tinel, Hanna, Delbeck, Martina, Mondritzki, Thomas, Wasnaire, Pierre, Dinh, Wilfried, Truebel, Hubert, Hüser, Jörg, Schmeck, Carsten

“…Increased plasma vasopressin levels have been shown to be associated with the progression of congestive heart failure. Vasopressin mediates water retention by…”
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Cholesteryl ester transfer protein and its inhibition by Weber, Olaf, Bischoff, Hilmar, Schmeck, Carsten, Böttcher, Michael-Friedrich

“…Cholesteryl ester transfer protein (CETP) is a plasma glycoprotein that facilitates the transfer of cholesteryl esters from the atheroprotective high density…”
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Improving the hit-to-lead process: data-driven assessment of drug-like and lead-like screening hits by Wunberg, Tobias, Hendrix, Martin, Hillisch, Alexander, Lobell, Mario, Meier, Heinrich, Schmeck, Carsten, Wild, Hanno, Hinzen, Berthold

“…We herein outline the usefulness of drug-like screening hits. As for lead-like hits it is of pivotal importance to have a detailed profile with experimental…”
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Novel tetrahydrochinoline derived CETP inhibitors by Schmeck, Carsten, Gielen-Haertwig, Heike, Vakalopoulos, Alexandros, Bischoff, Hilmar, Li, Volkhart, Wirtz, Gabriele, Weber, Olaf

“…Variations in the 4-position of 4 led to novel CETP inhibitors. The cyclohexyl group was found to be a suitable replacement for the pF-phenyl substituent…”
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In Silico ADMET Traffic Lights as a Tool for the Prioritization of HTS Hits by Lobell, Mario, Hendrix, Martin, Hinzen, Berthold, Keldenich, Jörg, Meier, Heinrich, Schmeck, Carsten, Schohe-Loop, Rudolf, Wunberg, Tobias, Hillisch, Alexander

“…The need for in silico characterization of HTS hit structures as part of a data‐driven hit‐selection process is demonstrated. A solution is described in the…”
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Chromanol derivatives—A novel class of CETP inhibitors by Vakalopoulos, Alexandros, Schmeck, Carsten, Thutewohl, Michael, Li, Volkhart, Bischoff, Hilmar, Lustig, Klemens, Weber, Olaf, Paulsen, Holger, Elias, Harry

“…A novel chemical class of active cholesteryl ester transfer protein (CETP) inhibitors were prepared and an evaluation of the structure–activity relationships…”
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Prediction of a potentially effective dose in humans for BAY 60–5521, a potent inhibitor of cholesteryl ester transfer protein (CETP) by allometric species scaling and combined pharmacodynamic and physiologically‐based pharmacokinetic modelling by Weber, Olaf, Willmann, Stefan, Bischoff, Hilmar, Li, Volkhart, Vakalopoulos, Alexandros, Lustig, Klemens, Hafner, Frank‐Thorsten, Heinig, Roland, Schmeck, Carsten, Buehner, Klaus

“…WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT • Cholesteryl ester transfer protein (CETP) is a plasma glycoprotein that facilitates the transfer of cholesteryl…”
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Single dose pharmacokinetics, pharmacodynamics, tolerability and safety of BAY 60–5521, a potent inhibitor of cholesteryl ester transfer protein by Boettcher, Michael‐Friedrich, Heinig, Roland, Schmeck, Carsten, Kohlsdorfer, Christian, Ludwig, Matthias, Schaefer, Anja, Gelfert‐Peukert, Sabine, Wensing, Georg, Weber, Olaf

“…WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT • Cholesteryl ester transfer protein (CETP) is a plasma glycoprotein that facilitates the transfer of cholesterol…”
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Differentiation of arginine vasopressin antagonistic effects by selective V2 versus dual V2/V1a receptor blockade in a preclinical heart failure model by Mondritzki, Thomas, Kolkhof, Peter, Sabbah, Hani N, Gheorghiade, Mihai, Fürstner, Chantal, Schmeck, Carsten, Siedentop, Harald, Schaefer, Stefan, Truebel, Hubert

“…Arginine vasopressin (AVP) is increased in patients with heart failure (HF). Its actions are linked to free water reabsorption (V2-) and arteriolar…”
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Novel heterocyclic thyromimetics. Part 2 by Haning, Helmut, Mueller, Ulrich, Schmidt, Gunter, Schmeck, Carsten, Voehringer, Verena, Kretschmer, Axel, Bischoff, Hilmar

“…Novel heterocyclic thyromimetics are presented carrying carboxy-substituted benzofurans or sulfur containing heterocycles, as replacements for the amino acid…”
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Stable Polymer-Bound Iodine Azide by Kirschning, Andreas, Monenschein, Holger, Schmeck, Carsten

“…1,2‐Azido‐iodination of a wide range of alkenes under very mild conditions can be achieved by using a novel iodate(I) reagent, a stable and storable…”
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Dibenzodioxocinones—A new class of CETP inhibitors by Brückner, David, Hafner, Frank-Thorsten, Li, Volkhart, Schmeck, Carsten, Telser, Joachim, Vakalopoulos, Alexandros, Wirtz, Gabriele

“…Dibenzodioxocinones with high inhibitory potential for CETP and good plasma stability were prepared by semisynthesis from a natural product precursor…”
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Novel heterocyclic thyromimetics by Haning, Helmut, Woltering, Michael, Mueller, Ulrich, Schmidt, Gunter, Schmeck, Carsten, Voehringer, Verena, Kretschmer, Axel, Pernerstorfer, Josef

“…The synthesis of novel heterocycle containing thyromimetics is reported. Potent indole thyromimetics are presented (e.g., 8) that show a 10-fold selectivity in…”
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