Zobrazeno 1 - 10
of 21
pro vyhledávání: '"Keith D. Barnes"'
Autor:
Graham Johnson, J. H. Lin, Jinhai Yang, Xinchao Chen, Steven L. Wagner, Nicholas J. Mayhew, R. Jason Herr, William C. Mobley, Kevin D. Rynearson, William D. Paquette, Keith D. Barnes, Rudolph E. Tanzi, Samuel A. Sakwa, Phuong Nguyen, Ronald N. Buckle
Publikováno v:
Bioorganic & medicinal chemistry, vol 28, iss 22
Bioorg Med Chem
Bioorg Med Chem
The evolution of gamma-secretase modulators (GSMs) through the introduction of novel heterocycles with the goal of aligning activity for reducing the levels of Aβ42 and properties consistent with a drug-like molecule are described. The insertion of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5b2a9db01bac416e5d7c90cd4e945c41
https://escholarship.org/uc/item/4ps6s92t
https://escholarship.org/uc/item/4ps6s92t
Autor:
Boglarka Racz, Keith D. Barnes, Enrique Michelotti, William H. Martin, Emily Freeman, Nicoleta Dobri, Christopher L. Cioffi, Charles L. Cywin, Douglas G. Stafford, Konstantin Petrukhin, Lei Zhu, Douglas B. Kitchen, Michael Conlon, Ping Chen, Paul G. Pearson, Daniel Schwarz, Graham Johnson
Publikováno v:
Journal of Medicinal Chemistry. 58:5863-5888
Antagonists of retinol-binding protein 4 (RBP4) impede ocular uptake of serum all-trans retinol (1) and have been shown to reduce cytotoxic bisretinoid formation in the retinal pigment epithelium (RPE), which is associated with the pathogenesis of bo
Autor:
Qiong Qin, Keith D. Barnes, Charles L. Cywin, Lei Zhu, Enrique Michelotti, Michael Conlon, Nicoleta Dobri, Paul G. Pearson, Christopher L. Cioffi, Boglarka Racz, Douglas B. Kitchen, Konstantin Petrukhin, Graham Johnson, Daniel M. C. Schwarz, William H. Martin, Ping Chen, Kathy C. Golden, Emily Freeman, Douglas G. Stafford
Publikováno v:
Journal of Medicinal Chemistry
Accumulation of lipofuscin in the retina is associated with pathogenesis of atrophic age-related macular degeneration and Stargardt disease. Lipofuscin bisretinoids (exemplified by N-retinylidene-N-retinylethanolamine) seem to mediate lipofuscin toxi
Autor:
Steven L. Wagner, Phuong Nguyen, R. Jason Herr, Nicholas J. Mayhew, Ronald N. Buckle, Rudolph E. Tanzi, Keith D. Barnes, William D. Paquette, Samuel A. Sakwa, Graham Johnson, Kevin D. Rynearson
Publikováno v:
Bioorganicmedicinal chemistry letters. 26(16)
The design and construction of a series of novel aminothiazole-derived γ-secretase modulators is described. The incorporation of heterocyclic replacements of the terminal phenyl D-ring of lead compound 1 was conducted in order to align potency with
Autor:
Menelas N. Pangalos, Jonathan A. Bard, Michael S. Malamas, Yinfa Yan, Jim Turner, Matthew D. Johnson, Ping Zhou, William Ronald Solvibile, Kristi Fan, Albert J. Robichaud, Yu Hui, Iwan Gunawan, Rajiv Chopra, Jim Erdei, Keith D. Barnes
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:5164-5170
The proteolytic enzyme β-secretase (BACE1) plays a central role in the synthesis of the pathogenic β-amyloid in Alzheimer’s disease. SAR studies of the S2′ region of the BACE1 ligand binding pocket with pyrazolyl and thienyl P2′ side chains a
Autor:
Chris Manley, Charles R. Heap, John Inthavongsay, Xuemei Chen, Yi Wang, Yiu-Yin Cheung, Ruifang Wang, Keith D. Barnes, Matthew D. Johnson, Bryan Duffy, Charles E. Schwartz, Ravi Krishnamoorthy, Melissa L. Allard, Stephan Steffke, Deepu Varughese
Publikováno v:
Tetrahedron Letters. 52:2623-2626
The enantioselective total synthesis of Resolvin E1 (RvE1), a naturally occurring small molecule mediator of inflammation resolution, is reported. Two routes are presented, both modular and convergent in nature, with an excellent control of all stere
Autor:
Ping Chen, Yingyan Chang, John W. Lippert, Yi Wang, Stephen H. Steffke, Christopher M. Manley, Keith D. Barnes, Guixing Wang, Robert M. Lewis, Nicholas J. Mayhew, Yuh-Lin A. Yang
Publikováno v:
Synthetic Communications. 41:67-72
A convergent synthesis of indoprofen via a Buchwald coupling approach is reported. Using this methodology, indoprofen and a set of analogs of indoprofen were readily prepared.
Autor:
Susan Salamone, Steven Tregay, Brian I. Bliss, Michael P. Trova, Simon Haydar, Joseph Anthony Bilotta, Luis Alicea, Patricia Snider, Matthew P. Rainka, R. Jason Herr, Xiaozhang Zheng, Denise Peace, Thuy Nguyen Duong, Keith D. Barnes, Travis Benanti, Thomas D. Friedrich, Matthew R. Johnson, Mark Bielaska, Yu Hui, John M. Lehman
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:6613-6617
The introduction of an aryl ring onto the 4-position of the C-6 benzyl amino group of the Cdk inhibitor roscovitine (2), maintained the potent Cdk inhibition demonstrated by roscovitine (2) as well as greatly improving the antiproliferative activity.
Autor:
Michael P. Trova, Keith D. Barnes, Curt Barford, Travis Benanti, Mark Bielaska, Lori Burry, John M. Lehman, Christine Murphy, Harold O’Grady, Denise Peace, Susan Salamone, Jennifer Smith, Patricia Snider, Joseph Toporowski, Steven Tregay, Alison Wilson, Michael Wyle, Xiaozhang Zheng, Thomas D. Friedrich
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:6608-6612
The introduction of an aryl ring onto the 4-position of the C-6 benzyl amino group of the Cdk inhibitor roscovitine (2), maintained the potent Cdk inhibition demonstrated by roscovitine (2) as well as greatly improving the antiproliferative activity.
Autor:
Jonathan A. Bard, Michael S. Malamas, Kristi Fan, Andrea Olland, Albert J. Robichaud, Erik Wagner, Yun Hu, Yu Hui, Iwan Gunawan, Jim Turner, Matthew R. Johnson, Jim Erdei, Keith D. Barnes
Publikováno v:
Journal of Medicinal Chemistry. 52:6314-6323
The identification of small molecule aminoimidazoles as potent and selective human beta-secretase inhibitors is reported. These analogues demonstrate low nannomolar potency for BACE1 in a FRET assay, exhibit comparable activity in a cell-based (ELISA