Zobrazeno 1 - 10
of 28
pro vyhledávání: '"Howard Roark"'
Autor:
Ron Sarver, Christopher Whitehead, Heidi Baum, James Hicks, Richard Gowan, Brian Sanchez, Xiao Kang Lu, Susan E. Bove, Joseph A. Cornicelli, Howard Miller, Sandra Lightle, Aurash B Shahripour, Katherine Welch, Craig Banotai, Jayvardhan Pandit, Mark S. Plummer, Timothy Braden, David Beidler, Adam Ogden, Skalitzky Donald James, Annise Paige Goodman, Howard Roark, Nalini Sadagopan, Charles J. Stankovic, Cindy Spessard, Xi Qiang Shen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:3438-3442
We identified potent, selective PDE2 inhibitors by optimizing residual PDE2 activity in a series of PDE4 inhibitors, while simultaneously minimizing PDE4 activity. These newly designed PDE2 inhibitors bind to the PDE2 enzyme in a cGMP-like mode in co
Autor:
Skalitzky Donald James, Craig Banotai, Jayvardhan Pandit, Adam Ogden, James Hicks, Annise Paige Goodman, Xiao Kang Lu, Howard Miller, Howard Roark, Susan E. Bove, Sandra Lightle, Aurash B Shahripour, Timothy Braden, Mark S. Plummer, Katherine Welch, Charles J. Stankovic, Ron Sarver, Joseph A. Cornicelli, Christopher Whitehead, Brian Sanchez, Nalini Sadagopan, Heidi Baum, Richard Gowan, David Beidler, Xi Qiang Shen, Cindy Spessard
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:3443-3447
Selective phosphodiesterase 2 (PDE2) inhibitors are shown to have efficacy in a rat model of osteoarthritis (OA) pain. We identified potent, selective PDE2 inhibitors by optimizing residual PDE2 activity in a series of phosphodiesterase 4 (PDE4) inhi
Autor:
Matthew Robert Johnson, Rajesh A. Shenoy, Van-Duc Le, Jolicia F. Gauuan, Howard Roark, James M. Hamby, Cheng Guo, Peter R. Guzzo, Michael Stier, John E. Mangette
Publikováno v:
Synthetic Communications. 41:2769-2793
As part of a medicinal chemistry collaboration, a number of novel bi- and tricyclic α-amino acids were prepared through various routes and characterized by 1H nuclear Overhauser effect difference experiments. The syntheses provide a number of routes
Autor:
Howard Roark, Matthew Robert Johnson, Michael Stier, Thomas Capiris, Peter R. Guzzo, Thomas Richard Belliotti, John E. Mangette, Van-Duc Le, Rajesh A. Shenoy
Publikováno v:
Tetrahedron. 65:9536-9541
Optically active α-amino 4H-[1,2,4]oxadiazol-5-ones (oxadiazolones) were prepared from optically active α-amino acids in five synthetic steps. The oxadiazolone moiety serves as a bioisosteric replacement for the carboxylic acid. Incorporation of an
Autor:
Dirk A. Bornemeier, Alexander Pavlovsky, Hyo-Kyung Han, Adam R. Johnson, Roberto N. De Guzman, Craig Banotai, Faith Prior, W. Howard Roark, Kaushik Datta, Patrick I. McConnell, Charles Lesch, W. Thomas Mueller, Richard D. Dyer, Chunhong Yan, Vijay Baragi, Daniel F. Ortwine, Michael D. Wilson, Chiu-Fai Man
Publikováno v:
Journal of Biological Chemistry. 282:27781-27791
Matrix metalloproteinase-13 (MMP13) is a Zn(2+)-dependent protease that catalyzes the cleavage of type II collagen, the main structural protein in articular cartilage. Excess MMP13 activity causes cartilage degradation in osteoarthritis, making this
Autor:
Howard Roark
On a trip to meet an ailing relative in Gangaikondacholapuram, Akash is introduced to conflict when a simple village girl, Ganga trespasses his thoughts. His mind fails to elude Ganga and, being overwhelmed by the new found emotion, his attempts to f
Autor:
Maureen K. Anderson, Reynold Homan, Joseph Armand Picard, R. L. Stanfield, Bruce D. Roth, Brian R. Krause, K. L. Hamelehle, W. Howard Roark, R. F. Bousley
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:2367-2370
A series of sulfonylureas were prepared and tested for the ability to inhibit the enzyme acyl-CoA: cholesterol acyltransferase (ACAT) in vitro and lower plasma cholesterol in cholesterol-fed rats in vivo. Although compounds from this series were gene
Autor:
Thomas Richard Belliotti, Rajesh A. Shenoy, Howard Roark, Van-Duc Le, Thomas Capiris, John E. Mangette, Peter R. Guzzo, Michael Stier, Matthew Robert Johnson
Publikováno v:
ChemInform. 41
Optically active α-amino 4H-[1,2,4]oxadiazol-5-ones (oxadiazolones) were prepared from optically active α-amino acids in five synthetic steps. The oxadiazolone moiety serves as a bioisosteric replacement for the carboxylic acid. Incorporation of an
Autor:
Brandon Collins, W. Howard Roark, Katherine E. Palmquist, Grace E. Munie, Mark E. Schnute, Olga V. Nemirovskiy, Patrick Michael Ann Arbor La Ann Arbor O'brien, Jeffrey A. Scholten, Karl W. Aston, Jeffery N. Carroll, Lillian E. Vickery, T. Sunyer, Steven L. Settle, Joe Nahra, Hanau Cathleen E, Bruce C. Hamper, Peter G. Ruminski, Patt William Chester, Jeffrey Hitchcock, Mark Morris, Huey S. Shieh, Theresa R. Fletcher, Chiu-Fai Man, Joseph J. McDonald, Adam R. Johnson, Michael David Rogers, Arthur J. Wittwer, Alexander Pavlovsky, Richard D. Dyer, Arun Agawal
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(2)
Potent, highly selective and orally-bioavailable MMP-13 inhibitors have been identified based upon a (pyridin-4-yl)-2H-tetrazole scaffold. Co-crystal structure analysis revealed that the inhibitors bind at the S(1)(') active site pocket and are not l
Autor:
Schnute, Mark E., O’Brien, Patrick M., Nahra, Joe, Morris, Mark, Howard Roark, W., Hanau, Cathleen E., Ruminski, Peter G., Scholten, Jeffrey A., Fletcher, Theresa R., Hamper, Bruce C., Carroll, Jeffery N., Patt, William C., Shieh, Huey S., Collins, Brandon, Pavlovsky, Alexander G., Palmquist, Katherine E., Aston, Karl W., Hitchcock, Jeffrey, Rogers, Michael D., McDonald, Joseph, Johnson, Adam R., Munie, Grace E., Wittwer, Arthur J., Man, Chiu-Fai, Settle, Steven L., Nemirovskiy, Olga, Vickery, Lillian E., Agawal, Arun, Dyer, Richard D., Sunyer, Teresa
Publikováno v:
In Bioorganic & Medicinal Chemistry Letters 2010 20(2):576-580