Zobrazeno 1 - 10
of 13
pro vyhledávání: '"Lizbeth, Gallagher"'
Autor:
Linda J Bristow, Amy E Easton, Yu-Wen Li, Digavalli V Sivarao, Regina Lidge, Kelli M Jones, Debra Post-Munson, Christopher Daly, Nicholas J Lodge, Lizbeth Gallagher, Thaddeus Molski, Richard Pieschl, Ping Chen, Adam Hendricson, Ryan Westphal, James Cook, Christiana Iwuagwu, Daniel Morgan, Yulia Benitex, Dalton King, John E Macor, Robert Zaczek, Richard Olson
Publikováno v:
PLoS ONE, Vol 11, Iss 7, p e0159996 (2016)
The development of alpha7 nicotinic acetylcholine receptor agonists is considered a promising approach for the treatment of cognitive symptoms in schizophrenia patients. In the present studies we characterized the novel agent, (2R)-N-(6-(1H-imidazol-
Externí odkaz:
https://doaj.org/article/cb2d80cbb97446c297511d2d30823d16
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:
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:
Valerie J. Whiterock, John E. Macor, Joanne J. Bronson, Melissa Hill-Drzewi, Regina Miller, Lizbeth Gallagher, Thaddeus F. Molski, Amy Easton, Xiaoliang Zhuo, Matthew D. Hill, Andrew P. Degnan, Xiaojun Han, Jeffrey M. Brown, Robert L. Bertekap, Haiquan Fang, Michael Gulianello, Michele Matchett, Kenneth S. Santone, Anand Balakrishnan
Publikováno v:
ACS Medicinal Chemistry Letters. 7:1082-1086
The metabotropic glutamate receptor 5 (mGluR5) is an attractive target for the treatment of schizophrenia due to its role in regulating glutamatergic signaling in association with the N-methyl-d-aspartate receptor (NMDAR). We describe the synthesis o
Autor:
Wilson Z. Shou, Lisa Elkin, Lizbeth Gallagher, Kathy Mosure, Matthew G. Soars, Andrew Dennis Wagner, Lindsey K. Stavola
Publikováno v:
Rapid Communications in Mass Spectrometry. 30:1787-1796
RATIONALE It is well known that the organic anion transporting polypeptide 1B1 (OATP1B1) plays a major role in the hepatic uptake of a range of drugs. To this end, it is pivotal that the potential for new molecular entities (NMEs) to inhibit OATP1B1
Autor:
Nicholas J. Lodge, John E. Macor, Matthew A. Seager, Samuel Gerritz, Shaun Langdon, Robert Zaczek, Joanne J. Bronson, Alda Fernandes, Karen Heman, James R. Merritt, Yuan Tian, Ryan Westphal, Yang Hong, Annapurna Pendri, Lizbeth Gallagher, Trevor Wojcik, Chongwu Zhang, Yu-Wen Li, Thaddeus F. Molski
Publikováno v:
Neuropharmacology. 102:121-135
Phosphodiesterase 10A (PDE10A) inhibitors increase the functionality of striatal medium spiny neurons and produce antipsychotic-like effects in rodents by blocking PDE10A mediated hydrolysis of cAMP and/or cGMP. In the current study, we characterized
Publikováno v:
Journal of Chromatography B. 967:211-218
A high throughput LC–MS/MS method for quantification of metformin substrate uptake enables conversion of radiometric transporter inhibition assays for multidrug and toxin extrusion transporters (MATE 1 and 2) and organic cation transporter 2 (OCT2)
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:
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