Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Jason Manka"'
Autor:
Jason Manka, Hilde Lavreysen, Colleen M. Niswender, Jon Jacobs, M. Luz Martín-Martín, P. Jeffrey Conn, Meredith J. Noetzel, Han Min Tong, Elizabeth J. Herman, C. David Weaver, Chrysa Malosh, J. Scott Daniels, Susana Conde-Ceide, Paige N. Vinson, Shaun R. Stauffer, Gregor James Macdonald, Claire Mackie, José Manuel Bartolomé-Nebreda, Thomas Steckler, Silvia López, Craig W. Lindsley, Carrie K. Jones, Satyawan Jadhav, Mark Turlington
Publikováno v:
Journal of Medicinal Chemistry. 57:5620-5637
Positive allosteric modulators (PAMs) of metabotropic glutamate receptor 5 (mGlu5) represent a promising therapeutic strategy for the treatment of schizophrenia. Starting from an acetylene-based lead from high throughput screening, an evolved bicycli
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ec9e09891e97fb3e6b29c5a56f045fdf
https://doi.org/10.1021/jm500259z
https://doi.org/10.1021/jm500259z
Autor:
P. Jeffrey Conn, Daryl F. Venable, Anna L. Blobaum, Jason Manka, Frank W. Byers, J. Scott Daniels, Colleen M. Niswender, Brittney S. Bates, Andrew S. Felts, Kyle A. Emmitte, Craig W. Lindsley, Alice L. Rodriguez, Carrie K. Jones, Ryan D. Morrison
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:5779-5785
Development of SAR in an aryl ether series of mGlu5 NAMs leading to the identification of tool compound VU0409106 is described in this Letter. VU0409106 is a potent and selective negative allosteric modulator of mGlu5 that binds at the known alloster
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6e9f7ffe0817814bcc13ec2e65816675
https://doi.org/10.1016/j.bmcl.2013.09.001
https://doi.org/10.1016/j.bmcl.2013.09.001
Autor:
Colleen M. Niswender, Anna L. Blobaum, Craig W. Lindsley, Jason Manka, Alice L. Rodriguez, P. Jeffrey Conn, Kyle A. Emmitte, J. Scott Daniels, Hyekyung P. Cho, Daryl F. Venable, Ryan D. Morrison
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:5091-5096
Development of SAR in an octahydropyrrolo[3,4-c]pyrrole series of negative allosteric modulators of mGlu1 using a functional cell-based assay is described in this Letter. The octahydropyrrolo[3,4-c]pyrrole scaffold was chosen as an isosteric replacem
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1007fd31f486ea3ef793ea8d5f409c8a
https://doi.org/10.1016/j.bmcl.2013.07.029
https://doi.org/10.1016/j.bmcl.2013.07.029
Autor:
Jason Manka, Thomas Steckler, Ya Zhou, Hilde Lavreysen, José M. Bartolomé, Elizabeth J. Herman, Karen J. Gregory, Colleen M. Niswender, Carrie K. Jones, Claire Mackie, P. Jeffrey Conn, Satya Jadhav, Kiran Gogi, Paige N. Vinson, C. David Weaver, Gregor James Macdonald, Emily Days, Shaun R. Stauffer, Richard Williams, J. Scott Daniels, Craig W. Lindsley
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:6481-6485
We report the optimization of a series of non-MPEP site metabotropic glutamate receptor 5 (mGlu(5)) positive allosteric modulators (PAMs) based on a simple acyclic ether series. Modifications led to a gain of MPEP site interaction through incorporati
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d534ec9be8ddffac91a13e546689a725
https://doi.org/10.1016/j.bmcl.2012.08.043
https://doi.org/10.1016/j.bmcl.2012.08.043
Publikováno v:
The Journal of Organic Chemistry. 69:1967-1971
Aryldiazo substituents were used in nucleophilic aromatic substitution reactions of halogens. The Ph-N=N- group activates ortho fluorine atoms toward alkylthiolation under mild conditions. In contrast, the Me(2)N-C(6)H(4)-N=N- group has virtually no
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a813ed153f666e552ef29ae85d70ab9f
https://doi.org/10.1021/jo0302399
https://doi.org/10.1021/jo0302399
Autor:
Monika J. Sienkowska, Fengli Guo, Piotr Kaszynski, Jason Manka, Vladimir Benin, Jianping Huang, Huiyong Yin, John M. Farrar
Publikováno v:
The Journal of Organic Chemistry. 68:9574-9588
A series of hexa- and octasubstituted biphenyls containing halogen, amino, nitro, and propylthio substituents were prepared by metal-mediated convergent synthesis from halobenzene precursors. The Pd-assisted C-C coupling methods were ineffective in t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d47c5f00cd8f18dd8d74101fa86771a0
https://doi.org/10.1021/jo030212p
https://doi.org/10.1021/jo030212p
Publikováno v:
The Journal of Organic Chemistry. 65:5202-5206
Several 5,6-disubstituted-7-oxabicyclo[2.2.1]hept-2-enes (1−4) were synthesized on ≥0.1 mol scale. The heat-induced retro Diels−Alder (rDA) decomposition of these derivatives was studied by thermal analysis, and the kinetics of the rDA were mea
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ef082ed34bc3fde0ae30123e619dc822
https://doi.org/10.1021/jo0003091
https://doi.org/10.1021/jo0003091
Autor:
Paige N. Vinson, Shaun R. Stauffer, Jason Manka, Zixiu Xiang, Craig W. Lindsley, P.J. Conn, Karen J. Gregory, Colleen M. Niswender, Meredith J. Noetzel
Metabotropic glutamate receptor 5 (mGlu5) is a target for the treatment of central nervous system (CNS) disorders, such as schizophrenia and Alzheimer’s disease. Furthermore, mGlu5 has been shown to play an important role in hippocampal synaptic pl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::64c435abc92520b83a64650e1f32562e
https://europepmc.org/articles/PMC3608436/
https://europepmc.org/articles/PMC3608436/
Autor:
Donald F. Stec, Alice L. Rodriguez, Ryan D. Morrison, Anna L. Blobaum, Roger Rush, Daryl F. Venable, Katrina A. Brewer, Andrew S. Felts, Thomas M. Bridges, P. Jeffrey Conn, Kyle A. Emmitte, Craig W. Lindsley, Melany M. Corlew, Colleen M. Niswender, Tammy S. Santomango, Frank W. Byers, J. Scott Daniels, Raymundo Sanchez-Ponce, Carrie K. Jones, Brittney S. Bates, Jason Manka
Negative allosteric modulation (NAM) of metabotropic glutamate receptor subtype 5 (mGlu5) represents a therapeutic strategy for the treatment of childhood developmental disorders, such as fragile X syndrome and autism. VU0409106 emerged as a lead com
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ed0389e68c022ccf3e9d93be7fbdaf65
https://europepmc.org/articles/PMC3422546/
https://europepmc.org/articles/PMC3422546/
Autor:
Carrie K. Jones, Jerri M. Rook, Meredith J. Noetzel, Zixiu Xiang, Colleen M. Niswender, P. Jeffrey Conn, Hyekyung P. Cho, Jason Manka, Rocco D. Gogliotti, Karen J. Gregory, Ya Zhou, F. Edward Dudek, Paige N. Vinson, Wendy A. Pouliot, Thomas M. Bridges, Shaun R. Stauffer, J. Scott Daniels, Craig W. Lindsley
Publikováno v:
Biological psychiatry. 73(6)
Background Metabotropic glutamate receptor subtype 5 (mGlu 5 ) activators have emerged as a novel approach to the treatment of schizophrenia. Positive allosteric modulators (PAMs) of mGlu 5 have generated tremendous excitement and fueled major drug d
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8ae1fdbe47c558b326c56fd37e54b0b4
https://pubmed.ncbi.nlm.nih.gov/23140665
https://pubmed.ncbi.nlm.nih.gov/23140665