Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Jeanette L. Bertron"'
Publikováno v:
The Journal of Organic Chemistry. 84:12187-12191
A concise formal total synthesis of pericoannosin A, by the synthesis of an advanced intermediate of pericoannosin A, was achieved in eight steps from commercially available isoprene in a 21.7% overall yield. Key transformations for this expedited ro
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8e4018ecc3827f9cd44bc78caeecf42c
https://doi.org/10.1021/acs.joc.9b01846
https://doi.org/10.1021/acs.joc.9b01846
Autor:
Alice L. Rodriguez, P. Jeffrey Conn, Allison R. Gregro, Michael Bubser, Mark E. Dugan, Colleen M. Niswender, Leah C. Konkol, Michael W. Wood, Darren W. Engers, Craig W. Lindsley, Jeanette L. Bertron, Bruce J. Melancon, Sean R. Bollinger, Thomas M. Bridges, Samantha E. Yohn, Vincent B. Luscombe, Andrew S. Felts, Michael R. Wood, Carrie K. Jones, Nicholas J. Brandon, Katrina A. Bollinger
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 29:1714-1718
This letter describes progress towards an M4 PAM preclinical candidate that resulted in the discovery of VU6005806/AZN-00016130. While the thieno[2,3-c]pyridazine core has been a consistent feature of key M4 PAMs, no work had previously been reported
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::49ea6005ae21bf03b498cfa06332687e
https://doi.org/10.1016/j.bmcl.2019.05.026
https://doi.org/10.1016/j.bmcl.2019.05.026
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:
Jonathan W. Dickerson, Anna L. Blobaum, Jerri M. Rook, Kellie D. Nance, Colleen M. Niswender, Shaun R. Stauffer, Craig W. Lindsley, Joel M. Harp, Hyekyung P. Cho, Sean P. Moran, James Maksymetz, Pedro M. Garcia-Barrantes, P. Jeffrey Conn, Carrie K. Jones, Daniel H. Remke, Jeanette L. Bertron, Sichen Chang
Publikováno v:
ACS Chemical Neuroscience. 9:2274-2285
Selective activation of the M(1) subtype of muscarinic acetylcholine receptor, via positive allosteric modulation (PAM), is an exciting strategy to improve cognition in schizophrenia and Alzheimer’s disease patients. However, highly potent M(1) ago
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::834d3641dcceed5eef09f3f3179e1e0c
https://doi.org/10.1021/acschemneuro.8b00131
https://doi.org/10.1021/acschemneuro.8b00131
Autor:
Shigenari Hayashi, Benjamin C. Tang, Jason E. Gestwicki, Xiaokai Li, Hao Shao, Daniel M. C. Schwarz, Jeanette L. Bertron
Publikováno v:
Bioorg Med Chem Lett
The molecular chaperone, Heat Shock Protein 70 (Hsp70), is an emerging drug target for neurodegenerative diseases, because of its ability to promote degradation of microtubule-associated protein tau (MAPT/tau). Recently, we reported YM-08 as a brain
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::20f8128df5ad8ab43fb7893c531574af
https://doi.org/10.1016/j.bmcl.2021.128025
https://doi.org/10.1016/j.bmcl.2021.128025
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:
Darren W, Engers, Bruce J, Melancon, Allison R, Gregro, Jeanette L, Bertron, Sean R, Bollinger, Andrew S, Felts, Leah C, Konkol, Michael R, Wood, Katrina A, Bollinger, Vincent B, Luscombe, Alice L, Rodriguez, Carrie K, Jones, Michael, Bubser, Samantha E, Yohn, Michael W, Wood, Nicholas J, Brandon, Mark E, Dugan, Colleen M, Niswender, P Jeffrey, Conn, Thomas M, Bridges, Craig W, Lindsley
Publikováno v:
Bioorganicmedicinal chemistry letters. 29(14)
This letter describes progress towards an M
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::cf31ffd80bc2a0d63aa6c41af28d67b3
https://pubmed.ncbi.nlm.nih.gov/33218899
https://pubmed.ncbi.nlm.nih.gov/33218899
Publikováno v:
ACS chemical neuroscience. 9(10)
Phencyclidine (PCP, "angel dust", an arylcyclohexylamine) was the first non-natural, man-made illicit drug of abuse, and was coined 'the most dangerous drug in America" in the late 1970s (amidst sensational horror stories of the drug's effects); howe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e5bb8ef053455407fbf7ba9ba57d27d8
https://pubmed.ncbi.nlm.nih.gov/29953199
https://pubmed.ncbi.nlm.nih.gov/29953199
Autor:
Jeanette L, Bertron, Hyekyung P, Cho, Pedro M, Garcia-Barrantes, Joseph D, Panarese, James M, Salovich, Kellie D, Nance, Darren W, Engers, Jerri M, Rook, Anna L, Blobaum, Colleen M, Niswender, Shaun R, Stauffer, P Jeffrey, Conn, Craig W, Lindsley
Publikováno v:
Bioorganicmedicinal chemistry letters. 28(12)
This letter describes the chemical optimization of a new series of M(1) positive allosteric modulators (PAMs) based on a novel benzomorpholine core, developed via iterative parallel synthesis, and culminating in the highly utilized rodent in vivo too
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::1daae11f6fe5dd151ccb5abc32a220bf
https://pubmed.ncbi.nlm.nih.gov/29754948
https://pubmed.ncbi.nlm.nih.gov/29754948
Autor:
Anna L. Blobaum, Jane Wright, Jerri M. Rook, Christopher J. Tarr, Jeanette L. Bertron, Jonathan W. Dickerson, Elizabeth A. Ennis, Charles W. Locuson, Craig W. Lindsley, Randy D. Blakely
Publikováno v:
Bioorganicmedicinal chemistry letters. 26(19)
This Letter describes the further lead optimization of the CHT inhibitor probe, ML352 (VU0476201), and the development of VU6001221, an improved in vivo tool. A multi-dimensional optimization effort encountered steep SAR, and ultimately, subtle tunin
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::38e22c48d72fc37a6a8b33b40b2f1515
https://pubmed.ncbi.nlm.nih.gov/27575469
https://pubmed.ncbi.nlm.nih.gov/27575469