Zobrazeno 1 - 10
of 23
pro vyhledávání: '"Kenneth P. Ellsworth"'
Autor:
Xinkang Wang, Dietmar Seiffert, Kenneth P. Ellsworth, Mark D. Erion, Xueping Zhou, Patrick Andre, Amjad Ali, Gino Castriota, Scott D. Edmondson, Stan Kurowski, David E. Gutstein, Zhu Chen, Donald Chu, Weizhen Wu, Lin Chu
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 360:476-483
Factor XI (FXI) is an integral component of the intrinsic pathway of the coagulation cascade and plays a critical role in thrombus formation. Because its role in the pathogenesis of cerebral microembolic signals (MES) is unclear, this study used a po
Autor:
Harold B. Wood, Kunal Desai, Daming Feng, Jamie McCabe-Dunn, Yi-Heng Chen, Edward C. Sherer, Jane Y. Wu, Marc Poirier, Hong Li, Dongfang Meng, Ting Zhang, Kenneth P. Ellsworth, Liangqin Guo, Teruyuki Nishimura, Jiayi Xu, Tomokazu Hirabayashi, Sunita V. Dewnani, Patrick Andre, Louis-Charles Campeau, Richard Tschirret-Guth, Isao Sakurada, Paul Reichert, Cameron J. Smith, Robert K. Orr, Lisa M. Sonatore, Wayne M. Geissler, Thomas Bateman, Kazuto Araki, Joe Metzger, Alan Hruza, Richard A. Berger, Dann L. Parker, Tianying Jian
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:5437-5443
Using structure based drug design, a novel class of potent coagulation factor IXa (FIXa) inhibitors was designed and synthesized. High selectivity over FXa inhibition was achieved. Selected compounds were evaluated in rat IV/PO pharmacokinetic (PK) s
Autor:
Edward C. Sherer, Susan E. Hill, Ian Knemeyer, Lisa M. Sonatore, Wayne M. Geissler, Peter J. Dandliker, Randal M. Bugianesi, Ting Zhang, Gary E. Martin, Xianshu Yang, Peter Nizner, Roy Helmy, Jackie Shang, Harold B. Wood, Kenneth P. Ellsworth, Huifang Yao, Yong Liu
Publikováno v:
Journal of medicinal chemistry. 59(5)
A potent and selective Factor IXa (FIXa) inhibitor was subjected to a series of liver microsomal incubations, which generated a number of metabolites. Using automated ligand identification system-affinity selection (ALIS-AS) methodology, metabolites
Autor:
Kenneth P. Ellsworth, M A Cleary, Gino Castriota, T F Vogt, Margaret Wu, Ruojing Yang, S Xu, Bei Zhang, Xiaodong Yang, M K Shin, Sajjad A. Qureshi, Yiping Chen, J-Lv Tran, Joel P. Berger
Publikováno v:
International Journal of Obesity (2005)
Objective: To investigate the impact of reduced adipocyte fatty acid-binding protein 4 (FABP4) in control of body weight, glucose and lipid homeostasis in diet-induced obese (DIO) mice. Methods: We applied RNA interference (RNAi) technology to genera
Autor:
Edward C. Sherer, Robert K. Orr, Wayne M. Geissler, Kazuto Araki, Thomas Bateman, Ting Zhang, Xiaoxia Qian, Kenneth P. Ellsworth, Teruyuki Nishimura, Andrew Nolting, Patrick Andre, Yi-Heng Chen, Paul Reichert, Kunal Desai, Harold B. Wood, Liangqin Guo, Dann L. Parker, Dongfang Meng, Cameron J. Smith, Lisa M. Sonatore, Tianying Jian, Richard Tschirret-Guth, Alan Hruza, Min Shu, Louis-Charles Campeau, Isao Sakurada
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(21)
Using structure based drug design (SBDD), a novel class of potent coagulation Factor IXa (FIXa) inhibitors was designed and synthesized. High selectivity over FXa inhibition was achieved. Selected compounds demonstrated oral bioavailability in rat IV
Autor:
Min Shu, William J. Greenlee, Alan Hruza, Harold B. Wood, Min Park, Shawn P. Walsh, Kenneth P. Ellsworth, Yi-Heng Chen, Lisa M. Sonatore, Bart Harper, Bing Li, Aurash Sharipour, Richard A. Berger, Cameron J. Smith, Esther Kim, Edward C. Sherer, Paul Reichert, Jane Y. Wu, Wayne M. Geissler, Jiayi Xu, Sunita V. Dewnani, James M. Balkovec, Dann L. Parker, Ting Zhang
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(11)
Two high-throughput screening hits were investigated for SAR against human factor IXa. Both hits feature a benzamide linked to a [6-5]-heteroaryl via an alkyl amine. In the case where this system is a benzimidazolyl-ethyl amine the binding potency fo
Autor:
Barbara Pio, Lyndon J. Mitnaul, Yan Guo, Gino Salituro, Harry R. Chobanian, Tesfaye Biftu, Joseph L. Duffy, Kim O’Neill, Kenneth P. Ellsworth, Nina Jochnowitz, Liangsu Wang, Jenna L. Terebetski, Lizbeth Hoos, Hong C. Shen, Yuchen Zhou, Mark A. Huffman, James D. Ormes, Brian Hawes, Dale Lewis, Maria Madeira
Publikováno v:
ACS medicinal chemistry letters. 6(5)
Modification of the previously disclosed (S)-N-(2-(aminomethyl)-5-chlorobenzyl)-1-((R)-2-hydroxy-3,3-dimethylbutanoyl)pyrrolidine-2-carboxamide 2 by optimization of the P3 group afforded novel, low molecular weight thrombin inhibitors. Heterocycle re
Autor:
Kenneth P. Ellsworth, Kevin T. Chapman, Wayne M. Geissler, Georgianna Harris, Robert W. Myers, Keith G. Rosauer, Anthony Ogawa, Qiaolin Deng, Christopher A. Willoughby, David E. Moller
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:4385-4388
The preparation of a series of substituted indoles coupled to six- and seven-membered cyclic lactams is described and their role as human glycogen phosphorylase a inhibitors discussed. The SAR of the indole moiety and lactam ring are presented.
Autor:
Kenneth P. Ellsworth, Robert W. Myers, Zhijian Lu, Richard Saperstein, Georgianna Harris, Brian M. McKeever, Wayne M. Geissler, Jun Yao, Kevin T. Chapman, Qiaolin Deng, Joann Bohn, Christopher A. Willoughby, Peggy E. McCann, Raynald Bergeron
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:4125-4128
A new class of diacid analogues that binds at the AMP site not only are very potent but have approximately 10-fold selectivity in liver versus muscle glycogen phosphorylase (GP) in the in vitro assay. The synthesis, structure, and in vitro and in viv
Autor:
Gool F. Patel, Ronald E. Painter, Wayne M. Geissler, Gayle E. Taylor, Georgianna Harris, Lynn L. Silver, Kenneth P. Ellsworth, Richard L. Tolman, Donald W. Graham, Amjad Ali, Katherine Young, Susan D. Aster
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:2185-2188
Substituted 2-amino-6-(anilino)pyrimidines have been found to be selective inhibitors of DNA polymerase III, a replicative enzyme known to be essential in the DNA synthesis of Gram-positive bacteria. Among the analogues, 18 displayed an IC50 of 10mM