Zobrazeno 1 - 10
of 102
pro vyhledávání: '"S, Kerwar"'
Autor:
Kwan Leung, Ken Rehder, Xiaofen Li, Bob Jiang, Marie Nguyen, Timothy A. Marquart, Nancy Chu, Victoria Y. Maydanik, David Lustig, Kevin D. Shenk, Yuan Li, Elfatih Elzein, Reina Natero, Daniel Soohoo, Prabha Ibrahim, Jeff Zablocki, Suresh S. Kerwar, Dmitry Koltun, Jia Hao, Dewan Zeng
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:6017-6021
New inhibitors of palmitoyl-CoA oxidation are based on the introduction of nitrogen heterocycles in the ‘Western Portion’ of the molecule. SAR studies led to the discovery of CVT-4325 (shown), a potent FOXi (IC50 = 380 nM rat mitochondria) with f
Autor:
Suresh S. Kerwar, Dov Shiffman, Eric E. Brooks, Nelson Marek G, Xingbo Wang, Xiaoming Zhang, Lum Robert T, Alison Joly, Michael M. Wick, Amy G. Horsma, Cheri Lynn Blum, Schow Steven R, Richard L. Mackman, Gavin Lee
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:2697-2702
The preparation of a series of 2,6,9-trisubstituted purines and the structure-activity data for the inhibition of cyclin dependent kinase, CDK2 are presented.
Autor:
F.L. Zhang, Suresh S. Kerwar, Walter C. Pickett, Michael M. Wick, Schow Steven R, C. Silverstrim
Publikováno v:
Analytical Biochemistry. 225:60-63
A new fluorescence assay for measuring the activity of geranylgeranyl transferase (type I) is described. It does not require the use of either radiolabeled geranylgeranyl diphosphate or the purified recombinant Ras protein substrate with the carboxy
Publikováno v:
Agents and Actions. 43:206-210
Rabbit inflamed synovial tissue grown in culture synthesizes a factor that induces collagenase synthesis in chondrocytes and in cartilage. Synthesis of this factor by the synovial tissue is inhibited by cycloheximide but not by indomethacin. The fact
Autor:
Robert E. Babine, Nan Zhang, Schow Steven R, Michael M. Wick, Martin F. Semmelhack, Richard C. Hastings, Zhangbao Xu, Suresh S. Kerwar, Randal A. Byrn
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:583-588
A new class of nonamino acid derived HIV-1 protease inhibitors of structure 1 are described. Structure activity relationships are discussed in the context of a protein crystal complex.
Autor:
Arnold L. Oronsky, Susan Quinn DeJoy, Walter C. Pickett, Lawrence W. Torley, Michael M. Wick, Suresh S. Kerwar, Robert Jeyaseelan, Allan Wissner
Publikováno v:
Journal of Infectious Diseases. 169:150-156
Experiments using a murine model of heat-killed Staphylococcus aureus-induced gram-positive bacterial sepsis indicate that the lethal bacterial effects can be prevented if mice are pretreated with CL 184,005, a platelet-activating factor (PAF) antago
Autor:
Schow Steven R, Suresh S. Kerwar, Michael M. Wick, Robert E. Babine, Randal A. Byrn, Bernard Dean Johnson, Michael R. Jirousek, Parimal R. Desai, Richard C. Hastings, Nan Zhang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 3:1589-1594
Lead compound 1, obtained from a previously reported structure-assisted design approach, was optimized to 17 using a traditional medicinal chemistry approach.
Autor:
Randal A. Byrn, Wellington T. Casscles, Michael M. Wick, Robert E. Babine, Schow Steven R, Nan Zhang, Grace C. Hsu, Bernard Dean Johnson, Michael R. Jirousek, Allan Wissner, Richard C. Hastings, Michael P. Trova, Suresh S. Kerwar
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 3:1595-1600
A series of HIV-1 protease inhibitors was prepared and evaluated against the free enzyme for inhibition properties, and for their anti-viral properties in human T lymphoid cells infected with HIVIIIB. Compounds 12, and 19 are the most potent anti-vir
Autor:
Michael P. Trova, Suresh S. Kerwar, Walter C. Pickett, Constance Kohler, Robert E. Schaub, Allan Wissner, Lawrence Wayne Torley, Marion L. Carroll
Publikováno v:
Journal of Medicinal Chemistry. 36:580-590
A series of platelet activating factor (PAF) antagonists containing a quaternary pyridinium ring connected through an amide, imide, or carbamate linkage to a substituted aromatic ring was prepared. Of these compounds, those containing a branched imid
Publikováno v:
International Journal of Antimicrobial Agents. 3:175-186
Since the isolation and elucidation of the structure of platelet-activating factor (PAF) in the late 1970's, several preclinical studies have suggested that PAF is a key mediator of septic shock induced in animals by either endotoxin or by Gram-negat