Zobrazeno 1 - 10
of 52
pro vyhledávání: '"Rodney A. Bednar"'
Autor:
Christine Fandozzi, James J. Vornov, Reza Mazhari, Scott D. Mosser, Shil Patel, Joseph J. Lynch, Nigel J. Liverton, Rachel M Garner, Rodney A. Bednar, Blake Paterson, John A. Mccauley, Shobha Gopalakrishnan, Stanley L. Gaul, Armando Lagrutta, Richard Briscoe, Laszlo Kiss
Publikováno v:
Pharmacology Research & Perspectives
The preclinical pharmacodynamic and pharmacokinetic properties of 4-methylbenzyl (3S, 4R)-3-fluoro-4-[(Pyrimidin-2-ylamino) methyl] piperidine-1-carboxylate (CERC-301), an orally bioavailable selective N-methyl-D-aspartate (NMDA) receptor subunit 2B
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::963a29e4d8bdaffca234948b39663662
http://europepmc.org/articles/PMC4777252
http://europepmc.org/articles/PMC4777252
Autor:
Nicole Trainor, E V Lis, Anthony G. DiLella, Terrence P. McDonald, Annie Liang, Mark E. Layton, Duane R. Reiss, Michael J. Kelly, Sanderson Philip E, James Yergey, Kevin J. Rodzinak, Steven D. Young, Guy R. Seabrook, Christine Fandozzi, Michael E. Cunningham, Scott D. Mosser, Mark O. Urban, John F. Fay, Hao Wang, Kenneth S. Koblan, Rodney A. Bednar
Publikováno v:
ACS Chemical Neuroscience. 2:352-362
A series of 3-substituted aminocyclopentanes has been identified as highly potent and selective NR2B receptor antagonists. Incorporation of a 1,2,4-oxadiazole linker and substitution of the pendant phenyl ring led to the discovery of orally bioavaila
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fd2684ec1a091b2da7e8fdaae9487129
https://doi.org/10.1021/cn200013d
https://doi.org/10.1021/cn200013d
Autor:
Scott D. Mosser, Joseph P. Vacca, Eric L. Moore, Rodney A. Bednar, Shane Roller, John F. Fay, Kathy M. Schirripa, Harold G. Selnick, Michael R. Wood, June J. Kim, Joseph G. Bruno, Christopher A. Salvatore
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:6827-6830
A previously utilized quinoline-for- N -phenylamide replacement strategy was employed against a central amide in a novel class of CGRP receptor antagonists. A unique and unexpected substitution pattern was ultimately required to maintain reasonable a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eec70e90291b9b8a02fdc7f9b0e97ab5
https://doi.org/10.1016/j.bmcl.2010.08.105
https://doi.org/10.1016/j.bmcl.2010.08.105
Autor:
Joseph P. Vacca, Eric L. Moore, Joseph G. Bruno, Craig A. Stump, Christopher A. Salvatore, Harold G. Selnick, Stefanie A. Kane, Amy G. Quigley, Rodney A. Bednar, Ian M. Bell, Kathy M. Schirripa, John F. Fay, Scott D. Mosser, Shane Roller, Michael R. Wood, June J. Kim
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5787-5790
A novel class of CGRP receptor antagonists was rationally designed by modifying a highly potent, but structurally complex, CGRP receptor antagonist. Initial modifications focused on simplified structures, with increased flexibility. Subsequent to the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3b8f1786a9f3caf835e3719393c88bbc
https://doi.org/10.1016/j.bmcl.2009.07.134
https://doi.org/10.1016/j.bmcl.2009.07.134
Autor:
Scott M. Doran, Kenneth E. Rittle, Yuxing Li, Cindy E. Nuss, Faith A. Mullen, Jeanine E. Ballard, Razvan Cristescu, Thomas S. Reger, Zhi-Qiang Yang, John J. Renger, Kenneth S. Koblan, Owen B. McManus, Vincent P. Santarelli, Rodney A. Bednar, Victor N. Uebele, Cuyue Tang, Susan L. Garson, Kelly-Ann S. Schlegel, Richard L. Kraus, Æ James C. Barrow, Ge Dai, Wei Lemaire, Steven V. Fox
Publikováno v:
Cell Biochemistry and Biophysics. 55:81-93
Low-voltage-activated (T-type) calcium channels play a role in diverse physiological responses including neuronal burst firing, hormone secretion, and cell growth. To better understand the biological role and therapeutic potential of the target, a nu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d29a9d226ba340e06a45f9ea741ba7e8
https://doi.org/10.1007/s12013-009-9057-4
https://doi.org/10.1007/s12013-009-9057-4
Autor:
John J. Renger, Chunze Li, Michael J. Bogusky, Yuxing Li, Scott M. Doran, David B. Whitman, Wei Lemaire, John D. Schreier, Joseph G. Bruno, Karen M. Brashear, Duane R. Reiss, Thomayant Prueksaritanont, Rodney A. Bednar, C. Meacham Harrell, Susan L. Garson, Paul J. Coleman, Richard L. Kraus, Christopher D. Cox, George D. Hartman, Kenneth S. Koblan, Michael J. Breslin, Christopher J. Winrow
Publikováno v:
ChemMedChem. 4:1069-1074
Silent Night: Antagonism of the orexin (or hypocretin) system has recently been identified as a novel mechanism for the treatment of insomnia. Herein, we describe discovery of a dual (OX(1)R/OX(2)R) orexin receptor antagonist featuring a 1,4-diazepan
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e66d6f4c7866f587c095e4844466f8a6
https://doi.org/10.1002/cmdc.200900069
https://doi.org/10.1002/cmdc.200900069
Autor:
Xu-Fang Zhang, Samuel L. Graham, Theresa M. Williams, Craig A. Stump, Victor K. Johnston, Scott D. Mosser, Joseph G. Bruno, C. Blair Zartman, Steven N. Gallicchio, Joseph P. Vacca, Eric L. Moore, Christopher A. Salvatore, John F. Fay, Rodney A. Bednar, Amy G. Quigley, Cory R. Theberge, Ian M. Bell, Stefanie A. Kane
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:214-217
Rational modification of a previously identified spirohydantoin lead structure has identified a series of potent spiroazaoxindole CGRP receptor antagonists. The azaoxindole was found to be a general replacement for the hydantoin that consistently imp
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ba289d690e0a68c717df88f7fd1e7e54
https://doi.org/10.1016/j.bmcl.2008.10.106
https://doi.org/10.1016/j.bmcl.2008.10.106
Autor:
Thomayant Prueksaritanont, Douglas J. Pettibone, Paul J. Coleman, Richard W. Ransom, Swati P. Mercer, Wei Lemaire, Kenneth S. Koblan, Jeffrey M. Bergman, Chunze Li, Anthony J. Roecker, Rodney A. Bednar, C. Meacham Harrell, Christopher J. Winrow, Kathy L. Murphy, Duane R. Reiss, George D. Hartman, John J. Renger
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:1425-1430
A series of OX2R/OX1R dual orexin antagonists was prepared based on a proline bis-amide identified as a screening lead. Through a combination of classical and library synthesis, potency enhancing replacements for both amide portions were discovered.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::00828baa8a3ff1ddc91122380369c298
https://doi.org/10.1016/j.bmcl.2008.01.001
https://doi.org/10.1016/j.bmcl.2008.01.001
Autor:
Jacquelynn J. Cook, Rodney A. Bednar, Thomayant Prueksaritanont, Yvonne M. Leonard, Michael R. Wood, Qin Mei, Richard W. Ransom, Ronald K. Chang, Emily D. Adarayn, Robert M. DiPardo, Jian Yu, Audrey A. Wallace, Wei Lemaire, Scott D. Kuduk, Kathy L. Murphy, G. R. Sitko, Scott D. Mosser, Christina N. Di Marco, Mark G. Bock, Frank C. Clayton, Bang-Lin Wan, Kathy M. Schirripa, Marie A. Holahan, Roger M. Freidinger, Dennis L. Bohn, Douglas J. Pettibone, Raymond S.L. Chang, Cuyue Tang, June J. Kim
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:716-720
Antagonism of the bradykinin B1 receptor represents a potential treatment for chronic pain and inflammation. Novel antagonists incorporating α-hydroxy amides were designed that display low-nanomolar affinity for the human bradykinin B1 receptor and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f489daa5ddd1907e6d600a79ad35db5d
https://doi.org/10.1016/j.bmcl.2007.11.050
https://doi.org/10.1016/j.bmcl.2007.11.050
Publikováno v:
JALA: Journal of the Association for Laboratory Automation. 8:54-63
We have automated in vitro dose-inhibition assays to evaluate newly synthesized chemical entities and to rapidly produce and disseminate the results with minimal personnel. A variety of assay methods were automated using the Tecan Genesis Workstation
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::b30ac50edbdb1c12334acf6eda4e5baf
https://doi.org/10.1016/s1535-5535-04-00281-3
https://doi.org/10.1016/s1535-5535-04-00281-3