Výsledky vyhledávání - "Jürgen Delzer"

Genomic Knockout of Endogenous Canine P-Glycoprotein in Wild-Type, Human P-Glycoprotein and Human BCRP Transfected MDCKII Cell Lines by Zinc Finger Nucleases

Autor: Masanori Tachikawa, Yasuo Uchida, Dominik Gartzke, Gert Fricker, Tetsuya Terasaki, Yutaro Hoshi, Jens Sydor, Loic Laplanche, Jürgen Delzer

Publikováno v: Pharmaceutical Research. 32:2060-2071

To investigate whether it is possible to specifically suppress the expression and function of endogenous canine P-glycoprotein (cPgp) in Madin-Darby canine kidney type II cells (MDCKII) transfected with hPGP and breast cancer resistance protein (hBCR

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3b1d7bffd528bb97ba89e7ffbf179647
https://doi.org/10.1007/s11095-014-1599-5

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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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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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Synthesis of highly potent and selective hetaryl ureas as integrin αVβ3-Receptor antagonists

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

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 12:1379-1382

Solid-phase synthesis and SAR of integrin alpha(V)beta3-receptor antagonists containing a urea moiety as non-basic guanidine mimetic are described. The most potent compounds exhibited IC(50) values towards alpha(V)beta3 in the nanomolar range and hig

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b393589d11872f1bdc969f5187bc92fb
https://doi.org/10.1016/s0960-894x(02)00161-0

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Synthesis and SAR of N-substituted dibenzazepinone derivatives as novel potent and selective αVβ3 antagonists

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

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 12:441-446

Synthesis and SARs of new integrin alpha(V)beta(3) antagonists based on an N-substituted dibenzazepinone scaffold are described. Variation of spacer and guanidine mimetic led to potent compounds exhibiting an IC(50) towards alpha(V)beta(3) in the nan

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e1b6f09fe12dd8f0abb5a7d457ffe91b
https://doi.org/10.1016/s0960-894x(01)00773-9

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A fluorescence-based in vitro assay for drug interactions with breast cancer resistance protein (BCRP, ABCG2)

Autor: Jürgen Delzer, Anne Mahringer, Gert Fricker

Publikováno v: European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V. 72(3)

Purpose: To establish a fluorescence-based assay for drug interactions with the ABC-export-protein BCRP (ABCG2). Methods: BCRP expression was verified by immunostaining and Western blots in intact porcine brain capillaries, isolated endothelial cells

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0ee37dc10d6e935ad12e8f4092dcc1ad
https://pubmed.ncbi.nlm.nih.gov/19572416

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Synthesis and SAR of highly potent and selective dopamine D3-receptor antagonists: variations on the 1H-pyrimidin-2-one theme

Autor: Liliane Unger, Linda L. King, Wilhelm Amberg, Gisela Backfisch, Armin Beyerbach, Hervé Geneste, Wilfried Braje, Charles W. Hutchins, Jürgen Delzer, Daryl R. Sauer, Wolfgang Wernet, Andreas Haupt

Publikováno v: Bioorganicmedicinal chemistry letters. 16(7)

In our efforts to further pursue one of the most selective dopamine D(3)-receptor antagonists reported to date, we now describe the synthesis and SAR of novel and highly selective dopamine D(3) antagonists based on a 1H-pyridin-2-one or on a urea sca

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b705136c87b970a57665195cccbbb4d6
https://pubmed.ncbi.nlm.nih.gov/16439127

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Synthesis and SAR of highly potent and selective dopamine D(3)-receptor antagonists: Quinolin(di)one and benzazepin(di)one derivatives. herve.geneste@abbott.com

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

Publikováno v: Bioorganicmedicinal chemistry letters. 16(3)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::49f0fc0c99b1fb936fc81abf3609b752
https://pubmed.ncbi.nlm.nih.gov/16271293

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