Zobrazeno 1 - 10
of 39
pro vyhledávání: '"Meredith J, Noetzel"'
Autor:
Shaun R. Stauffer, Rocco G. Gogliotti, P. Jeffrey Conn, Craig W. Lindsley, Carrie K. Jones, Thomas M. Bridges, Colleen M. Niswender, Karen J. Gregory, Meredith J. Noetzel
Publikováno v:
ACS Pharmacol Transl Sci
[Image: see text] Allosteric modulation of GPCRs represents an increasingly explored approach in drug development. Due to complex pharmacology, however, the relationship(s) between modulator properties determined in vitro with in vivo concentration-e
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::08b9357ed9a24f3cc9f07f77c38cda63
https://doi.org/10.1021/acsptsci.9b00062
https://doi.org/10.1021/acsptsci.9b00062
Autor:
Marianne K O Grant, Meredith J Noetzel, Kayla C De Lorme, Jan Jakubík, Vladimír Doležal, Esam E El-Fakahany
Publikováno v:
PLoS ONE, Vol 5, Iss 12, p e15722 (2010)
Xanomeline is a unique agonist of muscarinic receptors that possesses functional selectivity at the M(1) and M(4) receptor subtypes. It also exhibits wash-resistant binding to and activation of the receptor. In the present work we investigated the co
Externí odkaz:
https://doaj.org/article/fd8b3d721fb04aa3801c4db01a89e428
Autor:
Meredith J. Noetzel, Colleen M. Niswender, Jeanette L. Bertron, P. Jeffrey Conn, Alice L. Rodriguez, James C. Tarr, Michael W. Wood, Sichen Chang, Atin Lamsal, Thomas M. Bridges, Michael R. Wood, Rebecca L. Weiner, Carrie K. Jones, Mark E. Duggan, Hyekyung P. Cho, Craig W. Lindsley, Nicholas J. Brandon, Frank W. Byers
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:2990-2995
This letter details the continued chemical optimization of a novel series of M4 positive allosteric modulators (PAMs) based on a 5-amino-thieno[2,3-c]pyridazine core by incorporating a 3-amino azetidine amide moiety. The analogs described within this
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5c228f122a17fcbe5273cac4dc815cd8
https://doi.org/10.1016/j.bmcl.2017.05.014
https://doi.org/10.1016/j.bmcl.2017.05.014
Autor:
Changho Han, Eileen M. Engelberg, Michael R. Wood, Nicholas J. Brandon, Frank W. Byers, Darren W. Engers, Meredith J. Noetzel, Michael W. Wood, Hyekyung P. Cho, Sichen Chang, Craig W. Lindsley, Kellie D. Nance, Colleen M. Niswender, Atin Lamsal, Mark E. Duggan, Dedong Wu, Bruce J. Melancon, Carrie K. Jones, Thomas M. Bridges, Michael Bubser, P. Jeffrey Conn
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:2296-2301
This letter describes the further chemical optimization of the 5-amino-thieno[2,3-c]pyridazine series (VU0467154/VU0467485) of M4 positive allosteric modulators (PAMs), developed via iterative parallel synthesis, culminating in the discovery of the n
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::495b61beec721ee043d86e1cd8f2850a
https://doi.org/10.1016/j.bmcl.2017.04.043
https://doi.org/10.1016/j.bmcl.2017.04.043
Autor:
Michael R. Wood, Mark E. Duggan, Sichen Chang, Nicholas J. Brandon, Hyekyung P. Cho, James C. Tarr, Michael S. Poslusney, Michael Bubser, Atin Lamsal, Vincent B. Luscombe, Meredith J. Noetzel, Colleen M. Niswender, Rebecca L. Weiner, Craig W. Lindsley, P. Jeffrey Conn, Bruce J. Melancon, Darren W. Engers, Thomas M. Bridges, Carrie K. Jones, Michael W. Wood
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:171-175
This letter describes the chemical optimization of a novel series of M4 positive allosteric modulators (PAMs) based on a 5-amino-thieno[2,3-c]pyridazine core, developed via iterative parallel synthesis, and culminating in the highly utilized rodent i
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f3d2ea1c5ea4a6e91341513ff5e25c25
https://doi.org/10.1016/j.bmcl.2016.11.086
https://doi.org/10.1016/j.bmcl.2016.11.086
Autor:
Mark E. Duggan, Michael W. Wood, Michael R. Wood, Craig W. Lindsley, Vincent B. Luscombe, Miguel A. Hurtado, Bruce J. Melancon, Alice L. Rodriguez, Thomas M. Bridges, Atin Lamsal, Michael Bubser, Anna L. Blobaum, Carrie K. Jones, Meredith J. Noetzel, Darren W. Engers, Sichen Chang, Michael S. Poslusney, P. Jeffrey Conn, Rebecca L. Weiner, Nicholas J. Brandon, Kellie D. Nance, Colleen M. Niswender
Publikováno v:
ACS Medicinal Chemistry Letters. 8:233-238
Herein, we report the structure–activity relationships within a series of potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulators (PAMs). Compound 6c (VU0467485) possesses robust in vitro M
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f77e34fc69e38dff6d9f7e29757a3b53
https://doi.org/10.1021/acsmedchemlett.6b00461
https://doi.org/10.1021/acsmedchemlett.6b00461
Autor:
José Manuel Bartolomé-Nebreda, Thomas Steckler, Susana Conde-Ceide, Colleen M. Niswender, Chrysa Malosh, María Piedrafita, Meredith J. Noetzel, Claire Mackie, Paige N. Vinson, Jerri M. Rook, Gregor James Macdonald, M. Rosa Sánchez-Casado, P. Jeffrey Conn, Shaun R. Stauffer, Carlos M. Martínez-Viturro, Hilde Lavreysen, J. Scott Daniels, Carrie K. Jones, Mark Turlington, Thomas M. Bridges, Craig W. Lindsley
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:5115-5120
We report the optimization of a series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs) from an acyl dihydropyrazolo[1,5-a]pyrimidinone class. Investigation of exocyclic amide transpositions with this unique 5,6-bicy
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7b8088322559a22014da4ba8a0d907b9
https://doi.org/10.1016/j.bmcl.2015.10.009
https://doi.org/10.1016/j.bmcl.2015.10.009
Autor:
Carlos M. Martínez-Viturro, Colleen M. Niswender, Han Min Tong, Meredith J. Noetzel, Gregor James Macdonald, Susana Conde-Ceide, Carrie K. Jones, Claire Mackie, José Manuel Bartolomé-Nebreda, Thomas Steckler, P. Jeffrey Conn, Shaun R. Stauffer, Craig W. Lindsley, María Luz Martín-Martín, Thomas M. Bridges, J. Scott Daniels, Hilde Lavreysen, Silvia López, Sergio A. Alonso de Diego
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:1310-1317
We report the discovery and SAR of two novel series of imidazopyrimidinones and dihydroimidazopyrimidinones as metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs). Exploration of several structural features in the western
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e4a364a4c4741589a3db21524a2a658a
https://doi.org/10.1016/j.bmcl.2015.01.038
https://doi.org/10.1016/j.bmcl.2015.01.038
Autor:
P. Jeffrey Conn, Changho Han, Emery Smith, Colleen M. Niswender, Joseph D. Panarese, Craig W. Lindsley, Peter Hodder, Shaun R. Stauffer, Arindam Chatterjee, Peter Chase, Meredith J. Noetzel
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:384-388
Results from a 2012 high-throughput screen of the NIH Molecular Libraries Small Molecule Repository (MLSMR) against the human muscarinic receptor subtype 1 (M1) for positive allosteric modulators is reported. A content-rich screen utilizing an intrac
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::fbc10b64dbc431d6cac8193d33c7fb31
https://doi.org/10.1016/j.bmcl.2014.11.011
https://doi.org/10.1016/j.bmcl.2014.11.011
Autor:
Colleen M. Niswender, Meredith J. Noetzel, Michael R. Wood, Patrick R. Gentry, Peter Chase, Masaya Kokubo, Thomas M. Bridges, Emery Smith, P. Jeffrey Conn, Atin Lamsal, Craig W. Lindsley, Peter Hodder, J. Scott Daniels, Hyekyung P. Cho
Publikováno v:
Journal of Medicinal Chemistry
A functional high throughput screen identified a novel chemotype for the positive allosteric modulation (PAM) of the muscarinic acetylcholine receptor (mAChR) subtype 5 (M5). Application of rapid analog, iterative parallel synthesis efficiently optim
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9a8578211a3b76778d5cfff31f3e0501
https://doi.org/10.1021/jm500995y
https://doi.org/10.1021/jm500995y