Zobrazeno 1 - 10
of 27
pro vyhledávání: '"Helmut Mack"'
Autor:
Marjoleen Nijsen, Wilfried Hornberger, Achim Moeller, Volker Nimmrich, Helmut Mack, Andreas Kling, Katja Jantos, Yanbin Lao
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 29:1968-1973
Aberrant activation of calpain has been observed in various pathophysiological disorders including neurodegenerative diseases such as Alzheimer's Disease. Here we describe our efforts on ketoamide-based 1-benzyl-5-oxopyrrolidine-2-carboxamides as a n
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c4d6b168db54ba67ccee056772963483
https://doi.org/10.1016/j.bmcl.2019.05.034
https://doi.org/10.1016/j.bmcl.2019.05.034
Autor:
Adrian D. Hobson, Russell A. Judge, Ana L. Aguirre, Brian S. Brown, Yifang Cui, Ping Ding, Eric Dominguez, Enrico DiGiammarino, David A. Egan, Gail M. Freiberg, Sujatha M. Gopalakrishnan, Christopher M. Harris, Marie P. Honore, Karen L. Kage, Nicolas J. Kapecki, Christopher Ling, Junli Ma, Helmut Mack, Mulugeta Mamo, Stefan Maurus, Bradford McRae, Nigel S. Moore, Bernhard K. Mueller, Reinhold Mueller, Marian T. Namovic, Kaushal Patel, Steve D. Pratt, C. Brent Putman, Kara L. Queeney, Kathy K. Sarris, Lisa M. Schaffter, Vincent Stoll, Anil Vasudevan, Lei Wang, Lu Wang, William Wirthl, Kimberly Yach
Publikováno v:
Journal of Medicinal Chemistry. 61:11074-11100
A HTS campaign identified compound 1, an excellent hit-like molecule to initiate medicinal chemistry efforts to optimize a dual ROCK1 and ROCK2 inhibitor. Substitution (2-Cl, 2-NH
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ba127f0c7da3013553a7215d8180f4bd
https://doi.org/10.1021/acs.jmedchem.8b01098
https://doi.org/10.1021/acs.jmedchem.8b01098
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
https://doi.org/10.1021/acsmedchemlett.7b00494
Autor:
Wilfried Hornberger, Achim Moeller, Yanbin Lao, Kennan C. Marsh, Karla Drescher, Wicke Karsten, Andreas Kling, Ana Lucia Relo, Volker Nimmrich, Charles W. Hutchins, Katja Jantos, Helmut Mack
Publikováno v:
Journal of Medicinal Chemistry. 60:7123-7138
Calpain overactivation has been implicated in a variety of pathological disorders including ischemia/reperfusion injury, cataract formation, and neurodegenerative diseases such as Alzheimer's disease (AD). Herein we describe our efforts leading to th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c22512573f194ae025815e7aa3a15657
https://doi.org/10.1021/acs.jmedchem.7b00731
https://doi.org/10.1021/acs.jmedchem.7b00731
Publikováno v:
Macromolecular Reaction Engineering. 7:98-106
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3de4c8437e159824502f27e95b3b97a3
https://doi.org/10.1002/mren.201200040
https://doi.org/10.1002/mren.201200040
Autor:
Torben R. Neelands, Andrew O. Stewart, Gricelda H. Simler, Chengmin Zhong, Andrew J. King, Chang Z. Zhu, George Doherty, Andrew M. Swensen, Ivan Milicic, Janel M. Boyce-Rustay, Cenchen Zhan, Patricia N. Banfor, Timothy A. Vortherms, Victoria E. Scott, Natalie Bratcher, Michael F. Jarvis, Wende Niforatos, Helmut Mack, Pramila Bhatia
Publikováno v:
Biochemical Pharmacology. 83:406-418
Blockade of voltage-gated Ca²⁺ channels on sensory nerves attenuates neurotransmitter release and membrane hyperexcitability associated with chronic pain states. Identification of small molecule Ca²⁺ channel blockers that produce significant an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6e0e7b78ced7c8136433729efa16945e
https://doi.org/10.1016/j.bcp.2011.10.019
https://doi.org/10.1016/j.bcp.2011.10.019
Autor:
Wilfried Hornberger, Udo Lange, H. Wolfgang Hoeffken, Werner Seitz, Dorit Baucke, Helmut Mack
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:2641-2647
The synthesis and SAR of novel nanomolar thrombin inhibitors with the common backbone HOOC–CH2– d -cyclohexylalanyl-3,4-dehydroprolyl–NH–CH2–aryl-C( NH)NH2 are described together with their ecarin clotting time (ECT) prolongation as measure
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b0b1c22cb6af74974dd2b94358a05876
https://doi.org/10.1016/j.bmcl.2006.02.040
https://doi.org/10.1016/j.bmcl.2006.02.040
Autor:
Wicke Karsten, Liliane Unger, Achim Möller, Martin Schmidt, Udo Lange, Helmut Mack, Margot H. Bakker, Charles W. Hutchins, Wilfried Hornberger, Gerd Steiner, Kurt Schellhaas, Karla Drescher, Reinhold Müller, Andreas Kling
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:5567-5573
Novel 5-HT(1) autoreceptor ligands based on the N-4-aryl-piperazinyl-N'-ethyl-5,6,7,8-tetrahydropyrido[4', 3':4,5]thieno[2,3-d]pyrimidin-4(3H)-one core are described. Aiming at antidepressants with a novel mode of action our objective was to identify
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a2a0eb491929a50174dcc5475a6ac5f3
https://doi.org/10.1016/j.bmcl.2005.04.077
https://doi.org/10.1016/j.bmcl.2005.04.077
Publikováno v:
Nature Reviews Drug Discovery. 4:387-398
Rho kinases (ROCKs), the first Rho effectors to be described, are serine/threonine kinases that are important in fundamental processes of cell migration, cell proliferation and cell survival. Abnormal activation of the Rho/ROCK pathway has been obser
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0a9ec511ef92c015185281219539571d
https://doi.org/10.1038/nrd1719
https://doi.org/10.1038/nrd1719
Autor:
Bernd Schaefer, Thomas Zierke, Harald Bernard, Udo Lange, Helmut Mack, Werner Seitz, Thomas Pfeiffer, Gerd Buelow
Publikováno v:
Synthesis. 2004:2367-2375
In this account, we describe the development of an efficient and convergent process for the peptidomimetic thrombin inhibitor 1 on production plant scale. Starting from nicotinonitrile (13), (2S,4R)-1-(tert-butoxycarbonyl)-4-hydroxy-2-pyrrolidinecar-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::43552baa51dcef7a8013da4c2d9e3d6f
https://doi.org/10.1055/s-2004-831200
https://doi.org/10.1055/s-2004-831200