Výsledky vyhledávání - "Wolfgang Miltz"

Discovery of LYS006, a Potent and Highly Selective Inhibitor of Leukotriene A4 Hydrolase

Publikováno v: Journal of Medicinal Chemistry. 64:1889-1903

The cytosolic metalloenzyme leukotriene A4 hydrolase (LTA4H) is the final and rate-limiting enzyme in the biosynthesis of pro-inflammatory leukotriene B4 (LTB4). Preclinical studies have validated this enzyme as an attractive drug target in chronic i

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::208c74664f1cf048b5387b6f462e34b0
https://doi.org/10.1021/acs.jmedchem.0c01955

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Development of Selective, Orally Active GPR4 Antagonists with Modulatory Effects on Nociception, Inflammation, and Angiogenesis

Autor: Klaus Weigand, Andrea Vaupel, Roland Feifel, Berndt Oberhauser, Janet Dawson King, Mark Nash, Pius Loetscher, Amanda Littlewood-Evans, David Orain, Wolfgang Miltz, Juraj Velcicky

Publikováno v: Journal of Medicinal Chemistry. 60:3672-3683

A novel, selective, and efficacious GPR4 antagonist 13 was developed starting from lead compound 1a. While compound 1a showed promising efficacy in several disease models, its binding to a H3 receptor as well as a hERG channel prevented it from furth

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d140d7ef0960f3398069f19f6c5bc89f
https://doi.org/10.1021/acs.jmedchem.6b01703

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Feasibility and physiological relevance of designing highly potent aminopeptidase-sparing leukotriene A4 hydrolase inhibitors

Publikováno v: Scientific Reports
Scientific Reports, Vol 7, Iss 1, Pp 1-19 (2017)

Leukotriene A4 Hydrolase (LTA4H) is a bifunctional zinc metalloenzyme that comprises both epoxide hydrolase and aminopeptidase activity, exerted by two overlapping catalytic sites. The epoxide hydrolase function of the enzyme catalyzes the biosynthes

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c8c9381ec9ed6a6862eeaff01d18b6ec
https://doi.org/10.1038/s41598-017-13490-1

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Design and synthesis of potent and orally active GPR4 antagonists with modulatory effects on nociception, inflammation, and angiogenesis

Autor: Mark Nash, Janet Dawson, Arndt Meyer, Berndt Oberhauser, Klaus Seuwen, Juraj Velcicky, Pius Loetscher, Amanda Littlewood-Evans, Wolfgang Miltz, Daniela Gabriel, Marie-Gabrielle Ludwig, Roland Feifel

Publikováno v: Bioorganicmedicinal chemistry. 25(16)

GPR4, a G-protein coupled receptor, functions as a proton sensor being activated by extracellular acidic pH and has been implicated in playing a key role in acidosis associated with a variety of inflammatory conditions. An orally active GPR4 antagoni

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a8cc6c03181dbdf3b83e947377cef6b8
https://pubmed.ncbi.nlm.nih.gov/28689977

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A cassette-dosing approach for improvement of oral bioavailability of dual TACE/MMP inhibitors

Autor: Roland Feifel, Wolfgang Miltz, Ulf Neumann, Thomas Buhl, Philipp Janser

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 16:2632-2636

The structural features contributing to the different pharmacokinetic properties of the TACE/MMP inhibitors TNF484 and Trocade were analyzed using an in vivo cassette-dosing approach in rats. This enabled us to identify a new lead compound with excel

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https://doi.org/10.1016/j.bmcl.2006.02.042

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Determination of the active conformation of 6-amino-α-[(4-diphenylmethyl-1-piperazinyl)methyl-9H-purine]-9-ethanol: a positive inotropic agent

Autor: Roger Schultz, Wolfgang Miltz, Elena Buccheri, Wolfgang Zierhurt, Roger Stirnimann

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 3:1233-1239

Conformationally restricted analogues of the positive inotropic agent 1 have been synthesized in order to determine its biologically active conformation. Comparison of the distance maps (as a tool for the allowed conformations) with the biological ac

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::a35a617c6d45317259a6861dabee9774
https://doi.org/10.1016/s0960-894x(00)80322-4

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ChemInform Abstract: Reactions of N-Acyl-N-(2,2,2-trichloroethylidene)amines with Enamines

Autor: Wolfgang Steglich, Wolfgang Miltz

Publikováno v: ChemInform. 22

Title reaction with cyclic enamines affords chiral 2,2,2-trichloroethyl amine derivatives with high diastereo- and enantioselectivity.

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https://doi.org/10.1002/chin.199103137

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Targeting monocyte chemoattractant protein-1 signalling in disease

Autor: Wolfgang Miltz, Anis Mir, Christoph Wiessner, Janet Dawson

Publikováno v: Expert opinion on therapeutic targets. 7(1)

Monocyte chemoattractant protein-1 (MCP-1) has been implicated in many inflammatory and autoimmune diseases. The G-protein-coupled receptor CCR-2B is probably the most important MCP-1 receptor in vivo, and loss of MCP-1 effector function alone is suf

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eb9de1513c05fb32877d7fe5b0108c7c
https://pubmed.ncbi.nlm.nih.gov/12556201

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ChemInform Abstract: Methodology for the Enantioselective Synthesis of Aldols and Other 1,3-Dioxygenated Systems

Autor: Robert E. Ireland, Wolfgang Miltz, Benoit Vanasse, Peter Wipf

Publikováno v: ChemInform. 21

The enantioselective synthesis of the spiroenones 3, 4 from(S)-glycidol-O-benzyl ether and lithiated furan derivatives is described. After conjugate addition of lithium dimethyl cuprate or lithium divinyl cuprate and conversion of the resulting satur

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https://doi.org/10.1002/chin.199033189

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