Zobrazeno 1 - 10
of 55
pro vyhledávání: '"Paul E. Finke"'
Autor:
Weiguo Liu, Ramzi F. Sweis, Feroze Ujjainwalla, Remond Moningka, F. Anthony Romero, Yi Zang, Paul E. Finke, Zahid Hussain, Karen H. Dingley, Michael A. Plotkin, Andrew D. Howard, Jin Shang, Beth Ann Murphy, Jianming Bao, Gino Salituro, Harold B. Wood, Joseph L. Duffy
Publikováno v:
ACS Medicinal Chemistry Letters. 9:1088-1093
[Image: see text] A series of structurally diverse azaspirodecanone and spirooxazolidinone analogues were designed and synthesized as potent and selective somatostatin receptor subtype 5 (SSTR5) antagonists. Four optimized compounds each representing
Autor:
James G. Fox, Ki Taek Nam, Jared A. Weis, Nadia A. Ameen, James R. Goldenring, Victoria G. Weis, Paul E. Finke, Bonnie LaFleur, Josane F. Sousa
Publikováno v:
Gut. 62:1270-1279
Objectives Spasmolytic polypeptide-expressing metaplasia (SPEM) develops as a preneoplastic lesion in the stomachs of mice and humans after parietal cell loss. To identify the commonalities and differences between phenotypic SPEM lineages, SPEM were
Autor:
Ki Taek Nam, James R. Goldenring, Ryan L. O'Neal, Nick Barker, Robert J. Coffey, Paul E. Finke
Publikováno v:
Gut. 61:1678-1685
Objective Metaplastic lineages in the oxyntic mucosa of the stomach are critical preneoplastic precursors of gastric cancer. Recent studies have demonstrated that spasmolytic polypeptide-expressing metaplasia (SPEM) in the mouse oxyntic mucosa arises
The fibrinogen cleavage product A -Val360, a specific marker of neutrophil elastase activity in vivo
Autor:
Qian Si, Richard I Carter, Ali Ahmad, Richard A. Mumford, Asger Dirksen, Kelly M. Treonze, Robert A. Stockley, Paul E. Finke, P. Davies, John L. Humes, Eeva Piitulainen
Publikováno v:
Thorax. 66:686-691
Background Alpha-1-antitrypsin (A1AT) deficiency is the only recognised genetic risk factor for chronic obstructive pulmonary disease (COPD), a leading cause of morbidity and mortality worldwide. Since A1AT is the major inhibitor of neutrophil elasta
Autor:
D. Euan MacIntyre, Yue Feng, Lauren P. Shearman, Xiao-Ming Guan, Mark T. Goulet, Christopher W. Plummer, Sharon Tong, Quang Truong, D. Sloan Stribling, Donald J. Marsh, Junying Wang, Hong Yu, Kimberly Rosko, Sander G. Mills, Paul E. Finke, Alison M. Strack, Stephanie K. Spann, L. H. T. Van Der Ploeg, Shrenik K. Shah, Douglas J. MacNeil, Ramon E. Camacho, Joseph M. Metzger, William K. Hagmann, Tung M. Fong
Publikováno v:
European Journal of Pharmacology. 579:215-224
We document in vitro and in vivo effects of a novel, selective cannabinoid CB 1 receptor inverse agonist, Imidazole 24b (5-(4-chlorophenyl)- N -cyclohexyl-4-(2,4-dichlorophenyl)-1-methyl-imidazole-2-carboxamide). The in vitro binding affinity of Imid
Autor:
Gary G. Chicchi, Paul E. Finke, Joseph M. Metzger, Dorothy Levorse, Malcolm MacCoss, Margaret A. Cascieri, D. Euan MacIntyre, Laura C. Meurer, Kwei-Lan Tsao, Sharon Sadowski, Sander G. Mills
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:4497-4503
An initial investigation of the novel cyclopentane scaffold 6 afforded low nanomolar human NK1 antagonists having enhanced water solubility properties compared to morpholine 1. A synthesis of this cyclopentane scaffold, having three contiguous chiral
Autor:
Sander G. Mills, Xinchun Tong, Christopher W. Plummer, Chun-Pyn Shen, Jing Chen, Paul E. Finke, D. Sloan Stribling, Lex H.T. Van der Ploeg, George A. Doss, Junying Wang, Alison M. Strack, Lauren P. Shearman, Tung M. Fong, Julie Z. Lao, Marie-Therese Schaeffer
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:1441-1446
Structure–activity relationship studies directed toward the optimization of 4,5-diarylimidazole-2-carboxamide analogs as human CB1 receptor inverse agonists resulted in the discovery of the two amide derivatives 24a and b (hCB1 IC50 = 6.1 and 4.0 n
Autor:
Zhen Wang, Ronald B. Franklin, Paul E. Finke, Thomas A. Baillie, John R. Strauss, Su Er W Huskey, Shuet Hing L Chiu, William P. Feeney, Brian Dean, Bonnie Wang, Cornelis E. C. A. Hop, George A. Doss, Reza Anari, Minghua Zhang, Robichaud Albert Jean, P Cunningham
Publikováno v:
Drug Metabolism and Disposition. 32:246-258
The absorption, metabolism, and excretion of [14C]aprepitant, a potent and selective human substance P receptor antagonist for the treatment of chemotherapy-induced nausea and vomiting, was evaluated in rats and dogs. Aprepitant was metabolized exten
Autor:
M. Maccoss, Paul E. Finke, Bruce L. Daugherty, Youmin Weng, Di Salvo J, Julie A. DeMartino, Christopher L. Lynch, Laurie A. Castonguay, Marty S. Springer, J. J. Hale, Sander G. Mills, Adolfsen W, Charles G. Caldwell, Ruth Kilburn
Publikováno v:
Biochemistry. 42:1544-1550
The results of investigations in these laboratories of 2-aryl-4-(piperidin-1-yl)butanamines and 1,3,4-trisubstituted pyrrolidines as human CCR5 antagonists have recently been disclosed. To facilitate further development of these antagonists, we have
Autor:
William A. Schleif, Karen Holmes, Julie A. DeMartino, Liping Wang, Anthony Carella, Gwen Carver, Lorraine Malkowitz, Malcolm MacCoss, Paul E. Finke, Bryan Oates, Janet Lineberger, Emilio A. Emini, Ping Chen, Renee Danzeisen, Joseph Kessler, Michael W. Miller, Martin S. Springer, Sandra L. Gould, Daria J. Hazuda, Sander G. Mills, Dooseop Kim, Charles G. Caldwell
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:3099-3102
A series of hydantoin derivatives has been discovered as highly potent nonpeptide antagonists for the human CCR5 receptor. The synthesis, SAR, and biological profiles of this class of antagonists are described.