Zobrazeno 1 - 10
of 32
pro vyhledávání: '"Carleton R, Sage"'
Autor:
Thuy-Anh Tran, Bryan Kramer, Young-Jun Shin, Quyen-Quyen Do, Brett Ullman, Vasudeva Sagi, John W. Adams, Yunqing Shi, Hsin-Hui Shu, David J. Unett, Joel Gatlin, Michael E. Morgan, Jaimie Reuter, Anthony Blackburn, Carleton R. Sage, Graeme Semple
Publikováno v:
Results in Chemistry, Vol 4, Iss , Pp 100518- (2022)
The design of a new series of β3-Adrenergic receptor (β3-AdrR) antagonists is described. The use of a spiro building block in the core of the molecule provided novel compounds with reduced aromaticity and antagonist activity at the human β3-AdrR.
Externí odkaz:
https://doaj.org/article/6533cc49f4b54ba9916eb28cfabb9af8
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:
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:
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:
Dominic P. Behan, Kevin Whelan, Michael Morgan, Erin K. Sanabria, Andrew J. Grottick, Carleton R. Sage
Publikováno v:
Psychopharmacology
Rationale Synergistic or supra-additive interactions between the anorectics (dex)fenfluramine and phentermine have been reported previously in the rat and in the clinic. Studies with 5-HT2C antagonists and 5-HT2C knockouts have demonstrated dexfenflu
Autor:
Weichao Chen, Andrew M. Kawasaki, Dominic P. Behan, Jeff Edwards, You-An Ma, Tawfik Gharbaoui, Sun Hee Kim, Jayant Thatte, Hussien A. Al-Shamma, Carleton R. Sage, Jeremy Barden, Anthony C. Blackburn, Michelle Solomon, Xiuwen Zhu, Christopher Ronald J, David Mills, Ibragim Gaidarov, Antonio Garrido Montalban, Sangdon Han, Luis Lopez, Dipanjan Sengupta, Michael Morgan, Juerg Lehmann, Daniel J. Buzard, Graeme Semple, Kevin Whelan, Yinghong Gao, Joel Gatlin, Moody Jeanne, David J. Unett, Imelda Calderon, Lars Thoresen, Robert M. Jones, Brett Ullman, Todd Anthony, Chuan Chen, Minh Le, Khawja A. Usmani, Scott Stirn, Jaimie Karyn Rueter, Lixia Fu, Lorene Calvano, Abu J.M. Sadeque
Publikováno v:
ACS Medicinal Chemistry Letters. 5:1313-1317
APD334 was discovered as part of our internal effort to identify potent, centrally available, functional antagonists of the S1P1 receptor for use as next generation therapeutics for treating multiple sclerosis (MS) and other autoimmune diseases. APD3
Autor:
Antonio Garrido Montalban, Steve Chang, Shakya Sagar, P. Douglas Boatman, Weichao Chen, Dominic P. Behan, Thuy-Anh Tran, Yunqing Shi, Young-Jun Shin, Krishnan Ashwin M, Pureza Vallar, John W. Adams, David J. Unett, Michael Morgan, Bryan A. Kramer, Biman B. Pal, Hsin-Hui Shu, Anthony C. Blackburn, Juan Ramirez, Shiu-Feng Tung, Xiaohua Chen, Tina Leakakos, Ning Zou, Abu J.M. Sadeque, Tawfik Gharbaoui, Carleton R. Sage, Anna Shifrina, Graeme Semple, Ibragim Gaidarov
Publikováno v:
Journal of medicinal chemistry. 60(3)
The design and synthesis of a new series of potent non-prostanoid IP receptor agonists that showed oral efficacy in the rat monocrotaline model of pulmonary arterial hypertension (PAH) are described. Detailed profiling of a number of analogues result
Autor:
Jerry Xu, Milton L. Hammond, Brett Lauring, James R. Tata, Philip J. Skinner, Jens Knudsen, Daniel T. Connolly, Eseng Lai, Graeme Semple, Wen-Lin Luo, M. Gerard Waters, P. Douglas Boatman, John A. Wagner, Martin C. Cherrier, Jae-Kyu Jung, Steven L. Colletti, Andrew K.P. Taggart, Ester Carballo-Jane, Ruoping Chen, Benjamin R. Johnson, Thomas O. Schrader, Josee Cote, Carleton R. Sage, Luzelena Caro, Jeremy G. Richman, Michelle Kasem, Peter J. Webb
Publikováno v:
Journal of Medicinal Chemistry. 55:3644-3666
G-protein coupled receptor (GPCR) GPR109a is a molecular target for nicotinic acid and is expressed in adipocytes, spleen, and immune cells. Nicotinic acid has long been used for the treatment of dyslipidemia due to its capacity to positively affect
Autor:
Lixia Fu, Jeremy Barden, Joel Gatlin, Andrew M. Kawasaki, Minh Le, Jeff Edwards, Hussien A. Al-Shamma, Jayant Thatte, Charles Xing, Yinghong Gao, Moody Jeanne, Michelle Solomon, Sangdon Han, Carleton R. Sage, Thomas O. Schrader, Sheryll Espinola, Luis Lopez, Daniel J. Buzard, Ling Liu, Lars Thoresen, Robert M. Jones
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:6013-6018
S1P1 receptor driven lymphopenia has proven utility in the treatment of an array of autoimmune disease states. As a part of our efforts to develop potent and selective S1P1 receptor agonists, we have identified a novel chemical series of 4-oxo-4-(5-(
Publikováno v:
Journal of Chemical Information and Modeling. 51:1754-1761
Exploiting the ever growing set of activity data for compounds against biological targets represents both a challenge and an opportunity for ligand-based virtual screening (LBVS). Because G-protein coupled receptors (GPCRs) represent a rich set of po