Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Michelle, Kasem"'
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
Autor:
Ben Johnson, Tawfik Gharbaoui, Moody Jeanne, David J. Unett, Kevin Whelan, Ibragim Gaidarov, Michael Morgan, Lars Thoresen, Michelle Kasem, Abu J.M. Sadeque, Robert M. Jones, Chuan Chen, Sun Hee Kim, Hussien A. Al-Shamma, Minh Le, Joel Gatlin, Lorene Calvano, Andrew M. Kawasaki, Lixia Fu, Yinghong Gao, Scott Stirn, Weichao Chen, Jeremy Barden, Dominic P. Behan, Krishnan Ashwin M, Xiuwen Zhu, Graeme Semple, Dipanjan Sengupta, Christopher Ronald J, Jeff Edwards, Luis Lopez, Jayant Thatte, Daniel J. Buzard, Anthony C. Blackburn, Michelle Solomon, Todd Anthony, Thomas O. Schrader, Khawja A. Usmani
Publikováno v:
ACS Medicinal Chemistry Letters. 5:1334-1339
S1P1 is a validated target for treatment of autoimmune disease, and functional antagonists with superior safety and pharmacokinetic properties are being sought as second generation therapeutics. We describe the discovery and optimization of (7-benzyl
Autor:
Luis Lopez, Tawfik Gharbaoui, Daniel J. Buzard, Benjamin R. Johnson, Dipanjan Sengupta, Michelle Kasem, Robert M. Jones, Thomas O. Schrader, Christine Basmadjian
Publikováno v:
Organic Letters. 14:6306-6309
Two distinct and scalable enantioselective approaches to the tricyclic indole (R)-2-(7-hydroxy-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetate, an important synthon for a preclinical S1P(1) receptor agonist, are reported. Route 1 employs a modified v
Autor:
Thomas O, Schrader, Michelle, Kasem, Albert, Ren, Konrad, Feichtinger, Bilal, Al Doori, Jing, Wei, Chunrui, Wu, Huong, Dang, Minh, Le, Joel, Gatlin, Kelli, Chase, Jenny, Dong, Kevin T, Whelan, Carleton, Sage, Andrew J, Grottick, Graeme, Semple
Publikováno v:
Bioorganicmedicinal chemistry letters. 26(24)
The syntheses, structure-activity relationships (SARs), and biological activities of tetrahydroquinoline-based tricyclic amines as 5-HT