Zobrazeno 1 - 10
of 25
pro vyhledávání: '"F, Christopher Zusi"'
Autor:
Hyunsoo Park, James H. Cook, Ivar M. McDonald, Bradley C. Pearce, Matthew D. Hill, Haiquan Fang, John E. Macor, Lizbeth Gallagher, F. Christopher Zusi, Richard E. Olson, Linda J. Bristow
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:5002-5005
We describe an efficient and convergent synthesis of a series of (1'S,2R,4'S)-3H-4'-azaspiro[benzo[4,5]imidazo[2,1-b]oxazole-2,2'-bicyclo[2.2.2]octanes] displaying potency for the α7 nicotinic acetylcholine receptor (nAChR) and good selectivity vs.
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:
Valerie J. Whiterock, Amy Easton, Regina Miller, Lawrence R. Marcin, Meredith Ferrante, Bradley C. Pearce, John B. Hogan, Joanne J. Bronson, Clotilde Bourin, Mendi A. Higgins, Robert G. Gentles, F. Christopher Zusi, Walter Kostich, John E. Macor, Michael Gulianello, Min Ding, Linda J. Bristow, Adam Hendricson, Kim A. Johnson, Andrew Alt, Yanling Huang, Matthew A. Seager
Publikováno v:
Bioorganic & Medicinal Chemistry. 25:496-513
Triazolopyridine ethers with mGlu2 positive allosteric modulator (PAM) activity are disclosed. The synthesis, in vitro activity, and metabolic stability data for a series of analogs is provided. The effort resulted in the discovery of a potent, selec
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
Autor:
Daniel G. Morgan, Wendy Clarke, Nicholas J. Lodge, Yulia Benitex, John E. Macor, Debra J. Post-Munson, Ivar M. McDonald, Richard E. Olson, Dalton King, Rex Denton, Amy Easton, Ronald J. Knox, Kimberley A. Lentz, Christiana I. Iwuagwu, Matthew D. Hill, F. Christopher Zusi, Haiquan Fang, Robert Zaczek, Linda J. Bristow, Robert A. Mate, James H. Cook, Regina Miller
We describe the synthesis of quinuclidine-containing spiroimidates and their utility as α7 nicotinic acetylcholine receptor (nAChR) partial agonists. A convergent synthetic route allowed for rapid SAR investigation and provided a diverse set of fuse
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::46c72cac8d11dcb33041f5390751e60f
https://europepmc.org/articles/PMC5238485/
https://europepmc.org/articles/PMC5238485/
Autor:
Lizbeth Gallagher, Debra Post-Munson Amy Easton, Ivar M. McDonald, Dalton King, Nicholas J. Lodge, Regina Miller, Robert Zaczek, John E. Macor, James H. Cook, F. Christopher Zusi, Ronald J. Knox, Linda J. Bristow, Yulia Benitex, Judy Siuciak, Matthew D. Hill, Daniel G. Morgan, Robert A. Mate, Christiana I. Iwuagwu, Haiquan Fang, Richard E. Olson
Publikováno v:
Bioorganicmedicinal chemistry letters. 27(5)
Quinuclidine-containing spirooxazolines, as described in the previous report in this series, were demonstrated to have utility as α7 nicotinic acetylcholine receptor (α7 nAChR) partial agonists. In this work, the SAR of this chemotype was expanded
Autor:
Ivar M. McDonald, Robert A. Mate, Debra J. Post-Munson, Meredith Ferrante, David G. Harden, Lizbeth Gallagher, Richard E. Olson, F. Christopher Zusi, Barbara J. Robertson, Steven I. Dworetzky, Daniel G. Morgan, Hong Huang, Ronald J. Knox, Nicholas J. Lodge, John E. Macor, Robert L. Bertekap
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:1684-1688
High throughput screening led to the identification of a novel series of quinolone α7 nicotinic acetylcholine receptor (nAChR) agonists. Optimization of an HTS hit (1) led to 4-phenyl-1-(quinuclidin-3-ylmethyl)quinolin-2(1H)-one, which was found to
Autor:
Mendi A, Higgins, Lawrence R, Marcin, F, Christopher Zusi, Robert, Gentles, Min, Ding, Bradley C, Pearce, Amy, Easton, Walter A, Kostich, Matthew A, Seager, Clotilde, Bourin, Linda J, Bristow, Kim A, Johnson, Regina, Miller, John, Hogan, Valerie, Whiterock, Michael, Gulianello, Meredith, Ferrante, Yanling, Huang, Adam, Hendricson, Andrew, Alt, John E, Macor, Joanne J, Bronson
Publikováno v:
Bioorganicmedicinal chemistry. 25(2)
Triazolopyridine ethers with mGlu
Autor:
Kurt R. Gregor, Kim W. McIntyre, Carl Ouellet, Francis Beaulieu, Ruediger Edward H, Xuejie Yang, Yuping Qiu, Alain Martel, Dolatrai M. Vyas, Jacques Banville, F. Christopher Zusi, James R. Burke, Makonen Belema, John F. MacMaster, Mark A. Pattoli
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:1233-1237
We have recently identified BMS-345541 (1) as a highly selective and potent inhibitor of IKK-2 (IC50 = 0.30 μM), which however was considerably less potent against IKK-1 (IC50 = 4.0 μM). In order to further explore the SAR around the imidazoquinoxa
Autor:
Vojkan Susulic, Yuping Qiu, F. Christopher Zusi, David J. Shuster, Robert M. Townsend, Jennifer Postelnek, Kim W. McIntyre, James R. Burke
Publikováno v:
Transplantation. 77:1090-1094
BACKGROUND We previously demonstrated in vitro and in vivo that an IkappaB kinase (IKK) inhibitor blocks cytokine production and suppresses immune responses. These results indicate that a potent IKK inhibitor may have the potential of being a novel t