Zobrazeno 1 - 10
of 13
pro vyhledávání: '"Joseph Raymond Stock"'
Autor:
Cody Kelley, Marla Jean Williams, Kim Ji-In, Gregory J. Tawa, Katie Kubek, Joseph Raymond Stock, John W. Ellingboe, Thomas A. Comery, Suzan Aschmies, Warren D. Hirst, Brian J. Platt, William Ronald Solvibile, Xiaoping Ning, Jonathan Laird Gross, Albert J. Robichaud, Derek C. Cole
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:1237-1240
Using a focused screen of biogenic amine compounds we identified a novel series of H3R antagonists. A preliminary SAR study led to reduction of MW while increasing binding affinity and potency. Optimization of the physical properties of the series le
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9056c537f5642fa03e5ee54da0c7dc94
https://doi.org/10.1016/j.bmcl.2009.11.122
https://doi.org/10.1016/j.bmcl.2009.11.122
Autor:
Erik Wagner, Jonathan A. Bard, Kristine Svenson, Guixan Jin, Rajiv Chopra, Mei-Chu Lo, Minakshi Jani, Eric S. Manas, Pawel Nowak, Derek C. Cole, John W. Ellingboe, Baihua Hu, Robichaud Albert Jean, Kristi Fan, Michael S. Malamas, Rani Narasimhan, Jim Turner, Ann Aulabaugh, Ping Zhou, Rebecca Cowling, Steve Jacobsen, Peter H. Reinhart, Joseph Raymond Stock, Joan Subrath
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:632-635
8,8-Diphenyl-2,3,4,8-tetrahydroimidazo[1,5-a]pyrimidin-6-amine (1) was identified through HTS, as a weak (micromolar) inhibitor of BACE1. X-Ray crystallographic studies indicate the 2-aminoimidazole ring forms key H-bonding interactions with Asp32 an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2f64763182d742185f38a6b59ffe4de0
https://doi.org/10.1016/j.bmcl.2009.11.052
https://doi.org/10.1016/j.bmcl.2009.11.052
Autor:
M. James Turner, Lee D. Jennings, Ann Aulabaugh, Derek Cecil Cole, E.S. Manas, Mohani N. Sukhdeo, Steve Jacobsen, Joseph Raymond Stock, Laura Lin, James Strand, Junjun Wu, Mark L. Stahl, John W. Ellingboe, Guixan Jin, and Ping Zhou, Kristi Fan, Boyd L. Harrison, Rajiv Chopra, Kristine Svenson, Frank E. Lovering, Yun Hu, Erik Wagner, Jeffrey Scott Condon, Rebecca Cowling, Michael S. Malamas, Jonathan A. Bard
Publikováno v:
Journal of Medicinal Chemistry. 49:6158-6161
BACE1 is an aspartyl protease responsible for cleaving amyloid precursor protein to liberate Abeta, which aggregates leading to plaque deposits implicated in Alzheimer's disease. We have identified small-molecule acylguanidine inhibitors of BACE1. Cr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cd4ec479fdb92bb1e29c0bef451eeb32
https://doi.org/10.1021/jm0607451
https://doi.org/10.1021/jm0607451
Autor:
Lee E. Schechter, John W. Ellingboe, Deborah L. Smith, William Joseph Lennox, Joseph Raymond Stock, Derek C. Cole, Hossein Mazandarani, Guoming Zhang, Gregory J. Tawa
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:4780-4785
Several series of conformationally constrained N1-arylsulfonyltryptamine derivatives were prepared and tested for 5-HT6 receptor binding affinity and ability to modulate cAMP production in a cyclase assay. The 3-piperidin-3-yl-, 3-(1-methylpyrrolidin
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c73f46886c92daba6f420ae00deeef04
https://doi.org/10.1016/j.bmcl.2005.07.028
https://doi.org/10.1016/j.bmcl.2005.07.028
Publikováno v:
ChemInform. 33
A method has been developed for the oxidation of sulfides to sulfoxides on polystyrene resin. The polystyrene bound sulfoxide may be used in Swern oxidation reactions, and the used reagent may be regenerated by oxidation with tert-butylhydrogen perox
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::0e4debeded8974b4913a4d8d1a881dbc
https://doi.org/10.1002/chin.200249043
https://doi.org/10.1002/chin.200249043
Autor:
Peimin Lu, David S. Casebier, Dennis Kubrak, S. Aschmies, David Riddell, William Jay Moore, Zheng Wang, Mei Jin, Hua Zhou, Thomas A. Comery, John W. Ellingboe, Shaiu-Ching Sun, Erik Wagner, Aram Oganesian, Joseph Raymond Stock, Boyd L. Harrison, Zheng Xu, Robert Martone, George Diamantidis, Madelene Antane, Kevin Atchison, Kevin R. Woller, Yun Hu, June Sonnenberg-Reines, Charles William Mann, J. Steven Jacobsen, Anthony F. Kreft, Derek C. Cole
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(3)
Accumulation of beta-amyloid (Abeta), produced by the proteolytic cleavage of amyloid precursor protein (APP) by beta- and gamma-secretase, is widely believed to be associated with Alzheimer's disease (AD). Research around the high-throughput screeni
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2f145553716fc797084c8e75ab564dd0
https://pubmed.ncbi.nlm.nih.gov/19097890
https://pubmed.ncbi.nlm.nih.gov/19097890
Autor:
Hua Zhou, John W. Ellingboe, Derek Cecil Cole, Donna M. Huryn, Suzan Aschmies, Mei Jin, Charles William Mann, William E. Moore, Robert Martone, David S. Casebier, George Diamantidis, Zheng Xu, Alex Porte, Kevin R. Woller, Kevin Atchison, Anthony F. Kreft, Erik Wagner, Yun Hu, June Sonnenberg-Reines, Joseph T. Lundquist, J. Steven Jacobsen, Dennis Kubrak, Dave R. Riddell, Peimin Lu, Diane B. Hauze, Joseph Raymond Stock, Shaiu-Ching Sun, Boyd L. Harrison, Aram Oganesian
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(14)
Using a cell-based assay, we have identified a new series of Notch-sparing gamma-secretase inhibitors from HTS screening leads 2a and 2e. Lead optimization studies led to the discovery of analog 8e with improved gamma-secretase inhibitory potency and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2478e69d5a0c4998fbffb6b302c18ddb
https://pubmed.ncbi.nlm.nih.gov/18556202
https://pubmed.ncbi.nlm.nih.gov/18556202
Autor:
William Joseph Lennox, John W. Ellingboe, Deborah L. Smith, Derek Cecil Cole, Joseph Raymond Stock, and Chad E. Beyer, Louis Leung, Ronald C. Bernotas, Galante Rocco John, Pingzhong Huang, Lee A. Dawson, Michael F. Kelly, Steve Boikess, Xidong Feng, Lee E. Schechter, Karen L. Marquis, Sharon Rosenzweig-Lipson, Joseph Coupet, Guoming Zhang
Publikováno v:
Journal of medicinal chemistry. 50(23)
N1-Arylsulfonyltryptamines have been identified as 5-HT6 receptor ligands. In particular, N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine (11q) is a high affinity, potent full agonist (5-HT6 Ki = 2 nM, EC50 = 6.5 nM, Emax = 95.5%). Comp
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::110aa2ed2af7268ae0e0e06e3f3eefe1
https://pubmed.ncbi.nlm.nih.gov/17948978
https://pubmed.ncbi.nlm.nih.gov/17948978
Autor:
Andrea Olland, Jonathan A. Bard, Steve Jacobsen, John W. Ellingboe, Rebecca Cowling, Mary-Margaret O’Donnell, Junjun Wu, Joseph Raymond Stock, Kristine Svenson, Rajiv Chopra, Eric Wagner, Eric S. Manas, Lee D. Jennings, Michael S. Malamas, Robichaud Albert Jean, Yun Hu, Boyd L. Harrison, Kristi Fan, Derek C. Cole, William Jay Moore, Guixian Jin, Peter A. Lohse
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(3)
Proteolytic cleavage of amyloid precursor protein by beta-secretase (BACE-1) and gamma-secretase leads to formation of beta-amyloid (A beta) a key component of amyloid plaques, which are considered the hallmark of Alzheimer's disease. Small molecule
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e2bb91890c06c99491e6ceda30679c1c
https://pubmed.ncbi.nlm.nih.gov/18162398
https://pubmed.ncbi.nlm.nih.gov/18162398
Autor:
Hua Zhou, Diane B. Hauze, John W. Ellingboe, Robert Martone, Shaiu-Ching Sun, Dennis Kubrak, Alex Porte, David Riddell, Joseph Raymond Stock, Kevin Atchison, Susan Aschmies, Will Moore, Anthony F. Kreft, Boyd L. Harrison, Yun Hu, Kevin R. Woller, Charles William Mann, June Sonnenberg-Reines, Peimin Lu, Derek Cecil Cole, Steven Jacobsen, Donna M. Huryn, Mei Jin, Zheng Xu, Erik Wagner
Publikováno v:
Alzheimer's & Dementia. 2
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::8591d843baaef6a709c2f577d6dc4b07
https://doi.org/10.1016/j.jalz.2006.05.1984
https://doi.org/10.1016/j.jalz.2006.05.1984