Zobrazeno 1 - 10
of 22
pro vyhledávání: '"Joseph D, Panarese"'
Autor:
Corey R. Hopkins, Anna L. Blobaum, Joshua M. Wieting, Ryan Westphal, Rory A. Capstick, Alison R. Gregro, Julie E. Engers, Aspen Chun, P. Jeffrey Conn, Jason M. Guernon, Carrie K. Jones, Alice L. Rodriguez, Darren W. Engers, Joseph D. Panarese, Craig W. Lindsley, Wu Yong Jin, Joanne J. Bronson, John E. Macor, Andrew S. Felts, Kyle A. Emmitte, Colleen M. Niswender, Aaron M. Bender, Matthew Soars
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 29:342-346
This letter describes the first account of the chemical optimization (SAR and DMPK profiling) of a new series of mGlu4 positive allosteric modulators (PAMs), leading to the identification of VU0652957 (VU2957, Valiglurax), a compound profiled as a pr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::60fa1aa78e4f02203698c3a43924b7ed
https://doi.org/10.1016/j.bmcl.2018.10.050
https://doi.org/10.1016/j.bmcl.2018.10.050
Autor:
Jianming Yu, Jonathan Patrick Castillo, Michael H. J. Rhodin, Shook Brian C, Yat Sun Or, Nicole McAllister, Blaisdell Thomas P, Bryan Goodwin, In Jong Kim, Rachel Fearns, Kai Lin, Joseph D. Panarese, Sarah L. Noton
Publikováno v:
PLoS Pathogens, Vol 17, Iss 3, p e1009428 (2021)
PLoS Pathogens
PLoS Pathogens
EDP-938 is a novel non-fusion replication inhibitor of respiratory syncytial virus (RSV). It is highly active against all RSV-A and B laboratory strains and clinical isolates tested in vitro in various cell lines and assays, with half-maximal effecti
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d0a6592e56b65574881708ca316abf3f
https://doaj.org/article/4812af9d50bd47be8b478ee841cb733f
https://doaj.org/article/4812af9d50bd47be8b478ee841cb733f
Autor:
Michael J. Kates, Arlindo L. Castelhano, Carrie K. Jones, Colleen M. Niswender, Andrew S. Felts, Anna L. Blobaum, Matthew T. Loch, Kyle A. Emmitte, Aspen Chun, John E. Macor, Joanne J. Bronson, Darren W. Engers, Alice L. Rodriguez, Julie L. Engers, Joseph D. Panarese, Craig W. Lindsley, Michael A. Nader, Wu Yong Jin, P. Jeffrey Conn, Corey R. Hopkins
Publikováno v:
ACS Medicinal Chemistry Letters. 10:255-260
[Image: see text] Herein, we report the discovery of a novel potent, selective, CNS penetrant, and orally bioavailable mGlu(4) PAM, VU0652957 (VU2957, Valiglurax). VU2957 possessed attractive in vitro and in vivo pharmacological and DMPK properties a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9ad00e2611f409b59c25045eb5c2ba39
https://doi.org/10.1021/acsmedchemlett.8b00426
https://doi.org/10.1021/acsmedchemlett.8b00426
Autor:
Julie L. Engers, Alice L. Rodriguez, Analisa D. Thompson Gray, Corey R. Hopkins, Darren W. Engers, Anna L. Blobaum, Sean R. Bollinger, P. Jeffrey Conn, Colleen M. Niswender, Mary West, Carrie K. Jones, Joseph D. Panarese, Craig W. Lindsley, Matthew T. Loch
Publikováno v:
Journal of Medicinal Chemistry. 62:342-358
This work describes the discovery and characterization of novel 6-(1H-pyrazolo[4,3-b]pyridin-3-yl)amino-benzo[d]isothiazole-3-carboxamides as mGlu4 PAMs. This scaffold provides improved metabolic clearance and CYP1A2 profiles compared to previously d
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::18f31766602e34b5d54fdc293d180b2a
https://doi.org/10.1021/acs.jmedchem.8b00994
https://doi.org/10.1021/acs.jmedchem.8b00994
Autor:
John E. Macor, Darren W. Engers, Julie L. Engers, Colleen M. Niswender, P. Jeffrey Conn, Rocio Zamorano, Alice L. Rodriguez, Joanne J. Bronson, Sean R. Bollinger, Anna L. Blobaum, Joseph D. Panarese, Craig W. Lindsley, Alison R. Gregro, Corey R. Hopkins, Wu Yong Jin, Megan M. Breiner
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:2641-2646
Previous reports from our laboratory disclosed the structure and activity of a novel 1H-pyrazolo[4,3-b]pyridine-3-amine scaffold (VU8506) which showed excellent potency, selectivity and in vivo efficacy in preclinical rodent models of Parkinson’s d
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::390fa423031667d09c5d2e8b4064d1d9
https://doi.org/10.1016/j.bmcl.2018.06.034
https://doi.org/10.1016/j.bmcl.2018.06.034
The discovery of VU0486846: steep SAR from a series of M1 PAMs based on a novel benzomorpholine core
Autor:
Anna L. Blobaum, Jeanette L. Bertron, Jerri M. Rook, Kellie D. Nance, Colleen M. Niswender, Darren W. Engers, Pedro M. Garcia-Barrantes, P. Jeffrey Conn, James M. Salovich, Joseph D. Panarese, Craig W. Lindsley, Shaun R. Stauffer, Hyekyung P. Cho
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:2175-2179
This letter describes the chemical optimization of a new series of M1 positive allosteric modulators (PAMs) based on a novel benzomorpholine core, developed via iterative parallel synthesis, and culminating in the highly utilized rodent in vivo tool
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::1db77139d525d102e29fb8fd76dd2940
https://doi.org/10.1016/j.bmcl.2018.05.009
https://doi.org/10.1016/j.bmcl.2018.05.009
Autor:
Brandon A. Wright, Samuel Carlson, Elizabeth May, Vincent Chu, Petr Kuzmic, Shilpa Rani, Joseph D. Panarese, Rachelle Gaudet, Matthew D. Shair, Sreekanth Dittakavi, Danny T. C. Huang, Rocco L. Policarpo, Saravanakumar Dhakshinamoorthy, Aimo Kannt, Ludovic Decultot
Publikováno v:
J Med Chem
In this work, structure-based rational design led to the development of potent and selective alkynyl bisubstrate inhibitors of NNMT. The reported nicotinamide-SAM conjugate (named NS1) features an alkyne as a key design element that closely mimics th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4a04d8b7ae89b4cb800493a0e4df32f6
https://europepmc.org/articles/PMC7955893/
https://europepmc.org/articles/PMC7955893/
Autor:
Pedro M. Garcia-Barrantes, Colleen M. Niswender, J. Scott Daniels, Corey R. Hopkins, Rocco D. Gogliotti, P. Jeffrey Conn, Carrie K. Jones, Darren W. Engers, Analisa D. Thompson, Patrick R. Gentry, Anna L. Blobaum, Ryan D. Morrison, Joseph D. Panarese, Craig W. Lindsley
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:2915-2919
This letter describes the further chemical optimization of the picolinamide-derived family of mGlu4 PAMs wherein we identified a 3-amino substituent to the picolinamide warhead that engendered potency, CNS penetration and in vivo efficacy. From this
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a4dc481d0409d9d4782a26a5b56e1e94
https://doi.org/10.1016/j.bmcl.2016.04.041
https://doi.org/10.1016/j.bmcl.2016.04.041
Autor:
Joseph D, Panarese, Darren W, Engers, Yong-Jin, Wu, Jason M, Guernon, Aspen, Chun, Alison R, Gregro, Aaron M, Bender, Rory A, Capstick, Joshua M, Wieting, Joanne J, Bronson, John E, Macor, Ryan, Westphal, Matthew, Soars, Julie E, Engers, Andrew S, Felts, Alice L, Rodriguez, Kyle A, Emmitte, Carrie K, Jones, Anna L, Blobaum, P Jeffrey, Conn, Colleen M, Niswender, Corey R, Hopkins, Craig W, Lindsley
Publikováno v:
Bioorganicmedicinal chemistry letters. 29(2)
This letter describes the first account of the chemical optimization (SAR and DMPK profiling) of a new series of mGlu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::4f5a0723db9802aa8a0c09cb0a7f1d01
https://pubmed.ncbi.nlm.nih.gov/30503632
https://pubmed.ncbi.nlm.nih.gov/30503632
Autor:
Darren W, Engers, Sean R, Bollinger, Julie L, Engers, Joseph D, Panarese, Megan M, Breiner, Alison, Gregro, Anna L, Blobaum, Joanne J, Bronson, Yong-Jin, Wu, John E, Macor, Alice L, Rodriguez, Rocio, Zamorano, P Jeffrey, Conn, Craig W, Lindsley, Colleen M, Niswender, Corey R, Hopkins
Publikováno v:
Bioorganicmedicinal chemistry letters. 28(15)
Previous reports from our laboratory disclosed the structure and activity of a novel 1H-pyrazolo[4,3-b]pyridine-3-amine scaffold (VU8506) which showed excellent potency, selectivity and in vivo efficacy in preclinical rodent models of Parkinson's dis
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::e3947f5e3d34453d29a487fec5e7cb04
https://pubmed.ncbi.nlm.nih.gov/29958762
https://pubmed.ncbi.nlm.nih.gov/29958762