Zobrazeno 1 - 6
of 6
pro vyhledávání: '"Todd Andrew Brugel"'
Autor:
Gaochao Tian, William Frietze, Michael W. Wood, Christopher R. Holmquist, Todd Andrew Brugel, William E. Palmer, Hui Xiong, Deidre E. Wilkins, Glen Ernst, William Potts, Lindsay Hinkley, Janet Marie Forst, Xia Wang, Jeffrey S. Albert, Cristobal Alhambra, Gary Steelman, Jeffrey G. Varnes, Gerald Jonak, Don Andisik, Bruce Dembofsky, Chris Allan Veale
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:1043-1049
A series of isoquinuclidine benzamides as glycine uptake inhibitors for the treatment of schizophrenia are described. Potency, lipophilicity, and intrinsic human microsomal clearance were parameters for optimization. Potency correlated with the natur
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fc9dfd0d0aa8815e2e21d0c94b006632
https://doi.org/10.1016/j.bmcl.2018.02.029
https://doi.org/10.1016/j.bmcl.2018.02.029
Autor:
Linda C. Litwin, John C. Gordon, Anna Zacco, Carla Maciag, Timothy Piser, Todd Andrew Brugel, Carolann Thompson, Linda A. Sygowski, Matthew F. Peters, Patricia Schroeder
Publikováno v:
European Journal of Pharmacology. 661:27-34
The κ-opioid receptor plays a central role in mediating the response to stressful life events. Inhibiting κ-opioid receptor signaling is proposed as a mechanism for treating stress-related conditions such as depression and anxiety. Preclinical test
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f212aa26221789ed8dcadd08031d4557
https://doi.org/10.1016/j.ejphar.2011.04.017
https://doi.org/10.1016/j.ejphar.2011.04.017
Autor:
Michael Balestra, Francis M. McLaren, Julie Wilson, Linda A. Sygowski, Nathan Spear, James Kang, John P. McCauley, Lindsay Hinkley, Becky Brockel, Laura M. Panko, Valerie Hoesch, James Woods, Jalaj Arora, Kelly Brush, Minli Zhang, Thomas R. Simpson, Caprice Hightower, Dean G. Brown, Todd Andrew Brugel, Megan M. King, Abdelmalik Slassi, Vijay Chhajlani, Reed W. Smith, Gerard M. Koether, Reto Gadient, Hui Xiong, Methvin Isaac, Nathalie Breysse
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:7381-7384
Positive allosteric modulation of metabotropic glutamate receptor 5 (mGluR5) is regarded as a potential novel treatment for schizophrenic patients. Herein we report the synthesis and SAR of 4-aryl piperazine and piperidine amides as potent mGluR5 pos
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3d5646a25d7e6c272143c3c4c91c7174
https://doi.org/10.1016/j.bmcl.2010.10.036
https://doi.org/10.1016/j.bmcl.2010.10.036
Autor:
Reed W. Smith, Michael Balestra, Dean G. Brown, Todd Andrew Brugel, Gerard M. Koether, Christopher Becker, Laura M. Panko, John C. Gordon, Scott Throner, Matthew F. Peters, Ruifeng Liu, Thalia Daniels
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:5405-5410
Further structure activity relationship studies on a previously reported 8-azabicyclo[3.2.1]octan-3-yloxy-benzamide series of potent and selective kappa opioid receptor antagonists is discussed. Modification of the pendant N-substitution to include a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9f64b46019c11f71211f6ab144ce4e7b
https://doi.org/10.1016/j.bmcl.2010.07.112
https://doi.org/10.1016/j.bmcl.2010.07.112
Identification of N-(2-(azepan-1-yl)-2-phenylethyl)-benzenesulfonamides as novel inhibitors of GlyT1
Autor:
Deidre E. Wilkins, Jeffrey G. Varnes, Gerald Jonak, Christopher R. Holmquist, Gaochao Tian, Jeffrey S. Albert, Cristobal Alhambra, Tiffany N. Hoerter, Michael W. Wood, Todd Andrew Brugel, Janet Marie Forst, William Potts, Xia Wang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:4878-4881
A novel series of glycine transporter 1 (GlyT1) inhibitors is described. Scoping of the heterocycle moiety of hit 4-chlorobenzenesulfonamide 1 led to replacement of the piperidine with an azepane for a modest increase in potency. Phenyl sulfonamides
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8403805a07c4a4c264641e15948a1d48
https://doi.org/10.1016/j.bmcl.2010.06.085
https://doi.org/10.1016/j.bmcl.2010.06.085
Autor:
Laura M. Panko, Linda A. Sygowski, Patricia Schroeder, Matthew F. Peters, John C. Gordon, Anna Zacco, Scott Throner, Ruifeng Liu, Michael Balestra, Joseph Cacciola, Angela M. Hunter, James Folmer, Reed W. Smith, Thalia Daniels, Gerard M. Koether, Lee T. Hirata, Tiffany N. Hoerter, Dean G. Brown, Todd Andrew Brugel, Norman C. Ledonne, Mark Pietras, Philip D. Edwards, Christopher Becker
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(19)
Initial high throughput screening efforts identified highly potent and selective kappa opioid receptor antagonist 3 (κ IC50 = 77 nM; μ:κ and δ:κ IC50 ratios >400) which lacked CNS exposure in vivo. Modification of this scaffold resulted in devel
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1eb0a7172b07cd122fc6d93b09cbe19b
https://pubmed.ncbi.nlm.nih.gov/20727752
https://pubmed.ncbi.nlm.nih.gov/20727752