Zobrazeno 1 - 10
of 31
pro vyhledávání: '"Thomas O, Schrader"'
Autor:
Michael M. Poon, Kym I. Lorrain, Karin J. Stebbins, Geraldine C. Edu, Alexander R. Broadhead, Ariana O. Lorenzana, Bryanna E. Paulson, Christopher S. Baccei, Jeffrey R. Roppe, Thomas O. Schrader, Lino J. Valdez, Yifeng Xiong, Austin C. Chen, Daniel S. Lorrain
Publikováno v:
Scientific Reports, Vol 14, Iss 1, Pp 1-21 (2024)
Abstract Multiple sclerosis (MS) is a chronic neurological disease characterized by inflammatory demyelination that disrupts neuronal transmission resulting in neurodegeneration progressive disability. While current treatments focus on immunosuppress
Externí odkaz:
https://doaj.org/article/968e173534244880bfd928cf16265e56
Autor:
Daniel S. Lorrain, Ariana O Lorenzana, Alexander Broadhead, Christopher Baccei, Xiong Yifeng, Thomas O. Schrader, Michael M Poon, Karin J. Stebbins
Publikováno v:
ACS Medicinal Chemistry Letters. 12:155-161
The discovery of PIPE-359, a brain-penetrant and selective antagonist of the muscarinic acetylcholine receptor subtype 1 is described. Starting from a literature-reported M1 antagonist, linker replacement and structure-activity relationship investiga
Autor:
Thomas O, Schrader, Yifeng, Xiong, Ariana O, Lorenzana, Alexander, Broadhead, Karin J, Stebbins, Michael M, Poon, Christopher, Baccei, Daniel S, Lorrain
Publikováno v:
ACS Med Chem Lett
[Image: see text] The discovery of PIPE-359, a brain-penetrant and selective antagonist of the muscarinic acetylcholine receptor subtype 1 is described. Starting from a literature-reported M(1) antagonist, linker replacement and structure–activity
Autor:
Thomas O, Schrader, Xiuwen, Zhu, Michelle, Kasem, Albert, Ren, Chunyan, Liu, Chunrui, Wu, Huong, Dang, Minh, Le, Joel, Gatlin, Kelli, Chase, John, Frazer, Kevin T, Whelan, Andrew J, Grottick, Clayton, Hutton, Jeremy, Barden, Chuan, Chen, Alvaro, Ortiz, Konrad, Feichtinger, Graeme, Semple
Publikováno v:
Bioorganicmedicinal chemistry letters. 38
A series of novel (R)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,n]naphthyridines were identified as potent and selective agonists of the 5-HT
Autor:
Albert, Ren, Xiuwen, Zhu, Konrad, Feichtinger, Juerg, Lehman, Michelle, Kasem, Thomas O, Schrader, Amy, Wong, Huong, Dang, Minh, Le, John, Frazer, David J, Unett, Andrew J, Grottick, Kevin T, Whelan, Michael E, Morgan, Carleton R, Sage, Graeme, Semple
Publikováno v:
Bioorganicmedicinal chemistry letters. 30(5)
A series of potential new 5-HT
Autor:
Michelle Kasem, Graeme Semple, Sufang Li, Chunyan Liu, Albert S. Ren, Xiuwen Zhu, Thomas O. Schrader, Chunrui Wu
Publikováno v:
Tetrahedron Letters. 59:2030-2033
Asymmetric syntheses of N-protected (R)-4-halo-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,n]naphthyridines, advanced intermediates for the synthesis of highly potent and selective 5-HT2C agonists, are described. The key transformation involves ring
Autor:
Minh Le, Albert S. Ren, Andrew J. Grottick, Graeme Semple, Kevin Whelan, Kelli Chase, Carleton R. Sage, Bilal Al Doori, Jenny Dong, Michelle Kasem, Chunrui Wu, Konrad Feichtinger, Jing Wei, Thomas O. Schrader, Huong T. Dang, Joel Gatlin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:5877-5882
The syntheses, structure-activity relationships (SARs), and biological activities of tetrahydroquinoline-based tricyclic amines as 5-HT2C receptor agonists are reported. An early lead containing a highly unique 6,6,7-ring system was optimized for bot
Autor:
Clayton Hutton, Andrew J. Grottick, Graeme Semple, Konrad Feichtinger, Thomas O. Schrader, Jeremy Barden, Chunyan Liu, Kevin Whelan, Xiuwen Zhu, Chuan Chen, Chunrui Wu, John Frazer, Huong T. Dang, Joel Gatlin, Alvaro Ortiz, Minh Le, Albert S. Ren, Michelle Kasem, Kelli Chase
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 38:127872
A series of novel (R)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,n]naphthyridines were identified as potent and selective agonists of the 5-HT2C receptor. Optimizations performed on a previously reported series of racemic tetrahydroquinoline-based
Publikováno v:
Tetrahedron Letters. 57:4730-4733
Two distinct enantioselective approaches to (R)-2,3,4,4a,5,6-hexahydro-1H-pyrazino[1,2-a]quinolines and (R)-1,2,3,4,5,5a,6,7-octahydro-[1,4]diazepino[1,2-a]quinolines, low MW tricyclic organic scaffolds with a high degree of molecular complexity, are
Autor:
Albert S. Ren, Kevin Whelan, Konrad Feichtinger, Xiuwen Zhu, Michael Morgan, David J. Unett, Graeme Semple, Andrew J. Grottick, Amy Siu-Ting Wong, Michelle Kasem, Huong T. Dang, Juerg Lehman, Minh Le, Thomas O. Schrader, John Frazer, Carleton R. Sage
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 30:126929
A series of potential new 5-HT2 receptor scaffolds based on a simplification of the clinically studied, 5-HT2CR agonist vabicaserin, were designed. An in vivo feeding assay early in our screening process played an instrumental part in the lead identi