Výsledky vyhledávání - "Gisela Backfisch"

Mitigating the Metabolic Liability of Carbonyl Reduction: Novel Calpain Inhibitors with P1′ Extension

Autor: Marjoleen Nijsen, Katja Jantos, Helmut Mack, Wilfried Hornberger, Achim Moeller, Andreas Kling, Gisela Backfisch, Yanbin Lao, Beatrice Rendenbach-Mueller

Publikováno v: ACS Medicinal Chemistry Letters. 9:221-226

[Image: see text] Dysregulation of calpains 1 and 2 has been implicated in a variety of pathological disorders including ischemia/reperfusion injuries, kidney diseases, cataract formation, and neurodegenerative diseases such as Alzheimer’s disease

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::13bf1ef3c62188e81f6133eea6d3aaa4
https://doi.org/10.1021/acsmedchemlett.7b00494

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Enzymatic Late-Stage Oxidation of Lead Compounds with Solubilizing Biomimetic Docking/Protecting groups

Autor: Isabel Piel, Udo Lange, Gisela Backfisch, Clare Vickers, Frank Oellien

Publikováno v: Chemistry (Weinheim an der Bergstrasse, Germany). 24(68)

Late-stage functionalization of lead compounds is of high interest in drug discovery since it offers an easy access to metabolites and derivatives of a lead compound without the need to redesign an often long multistep synthesis. Owing to their high

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5fb3b0714b988280c6831033381ff55c
https://pubmed.ncbi.nlm.nih.gov/30451324

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In vitro Studies of Poorly Absorbed Drugs Using Porcine Intestine in the Ring Model RIMO

Autor: Richard Neidlein, Gisela Backfisch, Katja Nolte

Publikováno v: Arzneimittelforschung. 50:664-668

Two compounds, an aminobisphosphonate (A) and a steroid (B), showing a very large difference in lipophilicity (log PC (A) = O, log PC (B) > 8) but both revealing very poorly absorption in vivo of less than 1% were tested in respect of in vitro absorp

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f5240dbf47331d0e7d40cde4b12ea434
https://doi.org/10.1055/s-0031-1300269

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Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties

Autor: W. Lubisch, Astrid Netz, Wilfried Hornberger, Swati Bhowmik, Liliane Unger, Hervé Geneste, Wolfgang Wernet, Marcel M. van Gaalen, Thorsten Oost, Gisela Backfisch

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 21:3828-3831

Herein we report the discovery of a novel series of vasopressin 1b (V1b) receptor antagonists, starting from potent but metabolically labile oxindole SSR149415. Masking the proline N,N-dimethyl amide moiety as an oxazole and attaching a benzylic amin

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c4237a35b3d033a87a33d5c6c4dadf66
https://doi.org/10.1016/j.bmcl.2011.03.012

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Design and synthesis of novel potent and selective integrin αvβ3 antagonists—Novel synthetic routes to isoquinolinone, benzoxazinone, and quinazolinone acetates

Autor: Norbert Zimmermann, Jürgen Delzer, Andreas Kling, Gisela Backfisch, Thomas Subkowski, Hervé Geneste, Wilfried Hornberger, Claudia Isabella Graef, Werner Seitz

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 18:527-531

An unexpected ring contraction of benzazepinone based α v β 3 antagonists led to the design of quinolinone-type derivatives. Novel and efficient synthetic routes to isoquinolinone, benzoxazinone, and quinazolinone acetates were established. Nanomol

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b870c409473edd1250bdad4e5e3bcf53
https://doi.org/10.1016/j.bmcl.2007.11.089

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Synthesis and SAR of highly potent and selective dopamine D3-receptor antagonists: Quinolin(di)one and benzazepin(di)one derivatives

Autor: Andreas Haupt, Liliane Unger, Linda L. King, W. Lubisch, Gisela Backfisch, Hervé Geneste, Hans-Jürgen Teschendorf, Jürgen Delzer, Gerd Steiner, Charles W. Hutchins, Wilfried Braje, Wolfgang Wernet

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 16:658-662

The synthesis and SAR of novel and selective dopamine D(3)-receptor antagonists based on a 3,4-dihydro-1H-quinolin-2-one, a 1,3,4,5-tetrahydro-benzo[b]azepin-2-one, 1H-quinoline-2,4-dione or a 3,4-dihydro-1H-benzo[b]azepine-2,5-dione scaffold are dis

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::cb60071b7ee77e5d0fa8b2ac028ca37b
https://doi.org/10.1016/j.bmcl.2005.10.035

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Synthesis and SAR of highly potent and selective dopamine D3-receptor antagonists: 1H-Pyrimidin-2-one derivatives

Autor: Andreas Haupt, Jürgen Delzer, Hervé Geneste, Hans-Jürgen Teschendorf, Wilfried Braje, Andreas Kling, Liliane Unger, Wolfgang Wernet, Charles W. Hutchins, Linda L. King, Gisela Backfisch

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 16:490-494

The synthesis and SAR of novel highly potent and selective dopamine D(3)-receptor antagonists based on a 1H-pyrimidin-2-one scaffold are described. A-690344 antagonized PD 128907-induced huddling deficits in rat (ED(50) 6.1mg/kg po), a social interac

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5886a3b15b792f7b981616a10e1e86ef
https://doi.org/10.1016/j.bmcl.2005.10.068

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High-throughput quantitative and qualitative analysis of microsomal incubations by cocktail analysis with an ultraperformance liquid chromatography-quadrupole time-of-flight mass spectrometer system

Autor: Michael Schulz, Juliane Hoeckels-Messemer, Jonas Angstenberger, Beate Reder-Hilz, Gisela Backfisch, Jens Sydor, Loic Laplanche

Publikováno v: Bioanalysis. 7(6)

Background: Metabolite identification studies are very resource intensive and also are rarely performed in early discovery. Here, we report the validation of an ultraperformance liquid chromatography–high-resolution mass spectrometry (UPLC-HRMS) pl

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f9195ecc3f4e00e88bbb285a1d29dc93
https://pubmed.ncbi.nlm.nih.gov/25517264

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Highly potent and selective αVβ3-receptor antagonists: solid-phase synthesis and SAR of 1-substituted 4-amino-1H-pyrimidin-2-ones

Autor: Jürgen Delzer, Wilfried Hornberger, Christian Zechel, Gisela Backfisch, Thomas Subkowski, Andreas Kling, Werner Seitz, Claudia Isabella Graef, Udo E.W Lange, Hervé Geneste, Arnulf Lauterbach

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 13:165-169

Solid-phase synthesis and SAR of alpha(V)beta(3)-receptor antagonists based on a N(1)-substituted 4-amino-1H-pyrimidin-2-one scaffold are described. The most potent compounds exhibited IC(50) values towards alpha(V)beta(3) in the nano- to subnanomola

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f46b389f02a87c71234e971349a430b0
https://doi.org/10.1016/s0960-894x(02)00931-9

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