Zobrazeno 1 - 10
of 20
pro vyhledávání: '"David J. Cowan"'
Autor:
Lindsey T. Harston, David J. Cowan, Shane Roller, Caroline J. Diaz, Thomas J. Rimele, Channa K Jayawickreme, Paul Kenneth Spearing, Grace Chen, Claudia Generaux, Steven M. Sparks
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:4673-4677
Modulation of gastrointestinal nutrient sensing pathways provides a promising a new approach for the treatment of metabolic diseases including diabetes and obesity. The calcium-sensing receptor has been identified as a key receptor involved in minera
Autor:
Erin Swiger, Thomas J. Rimele, Vincent Rash, David Moncol, Donald L. Hertzog, Caroline J. Diaz, Jon L. Collins, Christopher Nystrom, Pierette Banker, David J. Cowan, Channa K Jayawickreme, Josephine Yuen, Sean Ross, Shane Roller, Xi Liang, Steven M. Sparks, Christopher Joseph Aquino, Dock Steven Thomas, Grace Chen
Publikováno v:
Bioorganicmedicinal chemistry letters. 27(5)
The long chain free fatty acid receptor 4 (FFA4/GPR120) has recently been recognized as lipid sensor playing important roles in nutrient sensing and inflammation and thus holds potential as a therapeutic target for type 2 diabetes and metabolic syndr
Autor:
Eric E. Boros, Robert L. Dobbins, Maggie S. McIntyre, Ryan Klein, David J. Cowan, Xi Liang, Xiaozhou Yao, Andrew A. Young, Kristin M. Patterson, Paul L. Feldman, John Ray, Christine L. Merrill, Lindsey T. Harston, Jeff L. Ambroso, Jon L. Collins, Shane Roller, Michael J. Bishop, Judith S. Prescott, Christopher Joseph Aquino, Alan Cunningham, Don L. Anderson, Istvan Kaldor, Wu Yulin, Lihong Chen, Josephine Yuen
Publikováno v:
Journal of Medicinal Chemistry. 56:5094-5114
The apical sodium-dependent bile acid transporter (ASBT) transports bile salts from the lumen of the gastrointestinal (GI) tract to the liver via the portal vein. Multiple pharmaceutical companies have exploited the physiological link between ASBT an
Autor:
Christie Schulte, Curt D. Haffner, J. Chuck Poole, Eric E. Boros, John C. Ulrich, David J. Cowan, Tiffany Carpenter, Eugene L. Stewart, J. Darren Stuart, Frank Preugschat, David N. Deaton, Tara Renae Rheault, Todd W. Shearer, Barry G. Shearer, J. David Becherer, Michael R. Jeune, Istvan Kaldor, Lisa M. Shewchuk, Terrence L. Smalley
Publikováno v:
Journal of medicinal chemistry. 58(17)
Starting from the micromolar 8-quinoline carboxamide high-throughput screening hit 1a, a systematic exploration of the structure-activity relationships (SAR) of the 4-, 6-, and 8-substituents of the quinoline ring resulted in the identification of ap
Autor:
John C. Ulrich, Petrov Kimberly, Tiffany Carpenter, David J. Cowan, J. Darren Stuart, J. David Becherer, Eugene L. Stewart, Frank Preugschat, David N. Deaton, W. Wallace Harrington, Yu Guo, Naphtali Milliken, Barry G. Shearer, Michael R. Jeune, Istvan Kaldor, Terrence L. Smalley, Curt D. Haffner, Brad R. Henke, Rodolfo Cadilla, Todd W. Shearer, Eric E. Boros, Christie Schulte
Publikováno v:
Journal of medicinal chemistry. 58(8)
A series of thiazoloquin(az)olinones were synthesized and found to have potent inhibitory activity against CD38. Several of these compounds were also shown to have good pharmacokinetic properties and demonstrated the ability to elevate NAD levels in
Autor:
M. Anthony Leesnitzer, Kimberly G. Petrov, Marcia L. Moss, Darryl Lynn Mcdougald, J. David Becherer, David J. Cowan, Robert W. Wiethe, Millard H. Lambert, David Lee Musso, Robert Andrews, D. Mark Bickett, Jennifer Gabriel Badiang, Michael D. Gaul, Andersen Marc W, Daniel B. Kassel, Michael H. Rabinowitz, R. Kevin Blackburn, Janet Warner, Daniel S. Kinder, Theresa D. Seaton
Publikováno v:
Combinatorial Chemistry & High Throughput Screening. 8:327-339
We report a systematic analysis of the P1' and P2' substrate specificity of TNF-alpha converting enzyme (TACE) using a peptide library and a novel analytical method, and we use the substrate specificity information to design novel reverse hydroxamate
Autor:
Eric E. Boros, Michael H. Rabinowitz, Lawrence A. Wolfe, James B. Thompson, Makda M. Mebrahtu, David J. Cowan, Richard F. Cox
Publikováno v:
The Journal of Organic Chemistry. 70:5331-5334
Small molecule calcitonin receptor agonists are of potential utility in the treatment and prevention of osteoporosis. Bicycloeneamine 1 was a useful intermediate in the synthesis of pyrazolopyridine calcitonin receptor partial agonists 2a-f. Dihydrop
Autor:
John A. Ray, Eric E. Boros, Mark B. Mitchell, Peter W. Sutton, Amy A. Sarjeant, Jon L. Collins, David J. Cowan
Publikováno v:
ChemInform. 45
A synthesis of the benzothiazepine phosphonic acid 3, employing both enzymatic and transition metal catalysis, is described. The quaternary chiral center of 3 was obtained by resolution of ethyl (2-ethyl)norleucinate (4) with porcine liver esterase (
Autor:
Jeffrey A. Stafford, Marcus F. Brackeen, Paul L. Feldman, James Marvin Veal, Margrith W. Verghese, Frank J. Schoenen, David J. Cowan, A. B. Strickland, D. Rose, Paul L. Domanico
Publikováno v:
Journal of Medicinal Chemistry. 38:4848-4854
The synthesis and biological evaluation of cAMP-specific phosphodiesterase (PDE IV) inhibitors is described. The PDE IV inhibitor 4-(3-butoxy-4-methoxybenzyl)imidazolidin-2-one (Ro 20-1724, 2) was used as a template from which to design a set of rigi
Autor:
Jeffrey A. Stafford, Alan B Strickland, D. Rose, Paul L. Domanico, Michael A. Leesnitzer, David J. Cowan, Rayomand J. Unwalla, Stephen A. Stimpson, Paul L. Feldman, Nicole L. Valvano, E Sloan Brawley, Margrith W. Verghese
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:1977-1982
Structure-activity relationships within a series of 1,3,4-trisubstituted pyrrolidines, novel and selective inhibitors of cAMP-specific phosphodiesterase (PDE IV), are discussed.