Zobrazeno 1 - 10
of 23
pro vyhledávání: '"Debra J. Post-Munson"'
Autor:
Carolyn Diane Dzierba, Debra J. Post-Munson, Ronald J. Knox, Lorin A. Thompson, Shuya Wang, Matthew G. Soars, Michele Matchett, Linda J. Bristow, James Herrington, Clotilde Bourin, Amy Newton, Rick L. Pieschl, Eric Shields, Amy Easton, Kathy Mosure, Guanglin Luo, Kimberly Newberry, Ling Chen, John D. Graef, Arun K. Senapati, Nicholas A. Meanwell, Digavalli V. Sivarao
Publikováno v:
Journal of Medicinal Chemistry. 62:831-856
3-Aryl-indole and 3-aryl-indazole derivatives were identified as potent and selective Nav1.7 inhibitors. Compound 29 was shown to be efficacious in the mouse formalin assay and also reduced complete Freund’s adjuvant (CFA)-induced thermal hyperalge
Autor:
David R. Langley, Rick L. Pieschl, John Watson, Simon Low, Linda J. Bristow, Debra J. Post-Munson, Michael K. Ahlijanian, Ramkumar Rajamani, Sophie Wu, James Herrington, Mian Gao, Lisa Megson, Iyoncy Rodrigo, David L. Wensel
Publikováno v:
Molecular Pharmacology. 92:310-317
The NaV1.7 voltage-gated sodium channel is implicated in human pain perception by genetics. Rare gain of function mutations in NaV1.7 lead to spontaneous pain in humans whereas loss of function mutations results in congenital insensitivity to pain. H
Autor:
Debra J. Post-Munson, Amy Easton, Carolyn Diane Dzierba, Amy Newton, Yong-Jin Wu, Ronald J. Knox, Kevin J. Robbins, Jason M. Guernon, Clotilde Bourin, Ramkumar Rajamani, Richard E. Olson, James Herrington, Michele Matchett, Kimberly Newberry, John D. Graef, Jianliang Shi, Lorin A. Thompson, Shuya Wang, Jonathan L. Ditta, Nicholas A. Meanwell, Rick L. Pieschl, Matthew G. Soars, Linda J. Bristow, Kathleen W. Mosure
Publikováno v:
Journal of Medicinal Chemistry. 60:2513-2525
By taking advantage of certain features in piperidine 4, we developed a novel series of cyclohexylamine- and piperidine-based benzenesulfonamides as potent and selective Nav1.7 inhibitors. However, compound 24, one of the early analogs, failed to red
Autor:
Regina Miller, Nicholas J. Lodge, John E. Macor, Wendy Clarke, Lizbeth Gallagher, Linda J. Bristow, Daniel G. Morgan, Christiana I. Iwuagwu, Ryan Westphal, Haiquan Fang, Kimberley A. Lentz, Debra J. Post-Munson, Amy Easton, Matthew D. Hill, Bei Wang, Robert A. Mate, Ivar M. McDonald, James H. Cook, Yulia Benitex, Dalton King, Thaddeus F. Molski, Ronald J. Knox, F. Christopher Zusi, Richard E. Olson, Rex Denton, Jingsong Fan, Rulin Zhao, Robert Zaczek
Publikováno v:
ACS Medicinal Chemistry Letters. 8:366-371
The therapeutic treatment of negative symptoms and cognitive dysfunction associated with schizophrenia is a significant unmet medical need. Preclinical literature indicates that α7 neuronal nicotinic acetylcholine (nACh) receptor agonists may provid
Autor:
Lizbeth Gallagher, Yulia Benitex, Matthew D. Hill, Richard E. Olson, Nicholas J. Lodge, Francine L. Healy, Debra J. Post-Munson, John E. Macor, Sivarao V. Digavalli, Daniel G. Morgan, JoAnne E Natale, Linda J. Bristow, Ping Chen, Haiquan Fang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:578-581
We describe the synthesis of quinuclidine-containing spiroguanidines and their utility as α7 neuronal nicotinic acetylcholine receptor (nAChR) partial agonists. The convergent synthetic route developed for this study allowed for rapid SAR investigat
Autor:
Guanglin, Luo, Ling, Chen, Amy, Easton, Amy, Newton, Clotilde, Bourin, Eric, Shields, Kathy, Mosure, Matthew G, Soars, Ronald J, Knox, Michele, Matchett, Rick L, Pieschl, Debra J, Post-Munson, Shuya, Wang, James, Herrington, John, Graef, Kimberly, Newberry, Digavalli V, Sivarao, Arun, Senapati, Linda J, Bristow, Nicholas A, Meanwell, Lorin A, Thompson, Carolyn, Dzierba
Publikováno v:
Journal of medicinal chemistry. 62(4)
Autor:
Ramkumar, Rajamani, Sophie, Wu, Iyoncy, Rodrigo, Mian, Gao, Simon, Low, Lisa, Megson, David, Wensel, Rick L, Pieschl, Debra J, Post-Munson, John, Watson, David R, Langley, Michael K, Ahlijanian, Linda J, Bristow, James, Herrington
Publikováno v:
Molecular pharmacology. 92(3)
The Na
Autor:
Yong-Jin, Wu, Jason, Guernon, Jianliang, Shi, Jonathan, Ditta, Kevin J, Robbins, Ramkumar, Rajamani, Amy, Easton, Amy, Newton, Clotilde, Bourin, Kathleen, Mosure, Matthew G, Soars, Ronald J, Knox, Michele, Matchett, Rick L, Pieschl, Debra J, Post-Munson, Shuya, Wang, James, Herrington, John, Graef, Kimberly, Newberry, Linda J, Bristow, Nicholas A, Meanwell, Richard, Olson, Lorin A, Thompson, Carolyn, Dzierba
Publikováno v:
Journal of medicinal chemistry. 60(6)
By taking advantage of certain features in piperidine 4, we developed a novel series of cyclohexylamine- and piperidine-based benzenesulfonamides as potent and selective Na
Autor:
Richard E. Olson, Ivar M. McDonald, Kimberly Newberry, Linda J. Bristow, Thaddeus F. Molski, Nicholas J. Lodge, Kelli M. Jones, Rick L. Pieschl, John E. Macor, Debra J. Post-Munson, Ryan Westphal, Ping Chen, Yu-Wen Li, Amy Easton, Yulia Benitex, Robert Zaczek, Yukiko Asaka, James Herrington, Siva Digavalli, Regina Miller, Daniel G. Morgan
Publikováno v:
European journal of pharmacology. 807
The α7 nicotinic acetylcholine receptor is thought to play an important role in human cognition. Here we describe the in vivo effects of BMS-902483, a selective potent α7 nicotinic acetylcholine receptor partial agonist, in relationship to α7 nico
Autor:
Regina Miller, Michele Matchett, Nicholas J. Lodge, Yulia Benitex, Thaddeus F. Molski, Wendy Clarke, John E. Macor, Rulin Zhao, Robert Zaczek, Linda J. Bristow, Amy Easton, Christiana I. Iwuagwu, JoAnne E Natale, Haiquan Fang, Ronald J. Knox, Baoqing Ma, F. Christopher Zusi, Siva Digavalli, James H. Cook, Matthew D. Hill, Francine L. Healy, Debra J. Post-Munson, Jingfang Qian Cutrone, Daniel G. Morgan, Bei Wang, Richard E. Olson, Qi Gao, Rex Denton, Robert A. Mate, Ivar M. McDonald, Dalton King, Meredith Ferrante, Kimberley A. Lentz, Kelli M. Jones, Judith A. Siuciak, Lizbeth Gallagher
Publikováno v:
Journal of medicinal chemistry. 59(24)
The design and synthesis of a series of quinuclidine-containing spirooxazolidines (“spiroimidates”) and their utility as α7 nicotinic acetylcholine receptor partial agonists are described. Selected members of the series demonstrated excellent se