Zobrazeno 1 - 10
of 17
pro vyhledávání: '"Joan A. Zugay"'
Publikováno v:
The Journal of organic chemistry. 58(5)
The synthesis of a differentially protected dipeptide mimic 10 in enantiomerically pure form is described. The key step involves the epimerization of the C-2 center of the lactone 4, hydrolysis and protection of the resulting hydroxy acid, followed b
Autor:
Joseph P. Vacca, Joan A. Zugay, B. E. Evans, William A. Schleif, B. Moon Kim, Emilio A. Emini, Jiunn H. Lin, Kari Vastag, Paul L. Darke, Stuart R. Michelson, I.-W. Chen, Kevin F. Gilbert, Joel R. Huff, Colleen M. Hanifin, P. S. Anderson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:2707-2712
A series of HIV-1 protease inhibitors containing various acyclic or cyclic alkylpiperazine derivatives were prepared. They exhibit excellent potency in the enzyme inhibition assay and in a whole cell assay demonstrating the lowest CIC 95 IC 50 ratios
Autor:
Colleen M. Hanifin, Joel R. Huff, William A. Schleif, Jiunn H. Lin, P. S. Anderson, Emilio A. Emini, C. Blair Zartman, I.-W. Chen, B. Moon Kim, Joan A. Zugay, Joseph P. Vacca, Paul L. Darke, Stuart R. Michelson, Kari Vastag
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:2239-2244
As a systematic approach to develop HIV-1 protease inhibitors exhibiting desirable pharmacokinetic profiles, hydroxyethylpiperazine series of inhibitors containing various mono- or dialkyl-substituted pyridylmethyl groups have been examined. Very hig
Autor:
Kari Vastag, P. S. Anderson, I.-W. Chen, Joan A. Zugay, Joel R. Huff, James P. Guare, Joseph D. Vacca, Emilio A. Emini, Paul L. Darke, Stuart R. Michelson, B. Moon Kim, William A. Schleif, Jiunn H. Lin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:185-190
A series of hydroxyethylpiperazine HIV-1 protease inhibitors containing various monocyclic or bicyclic thienylmethyl substituents as P3′ ligands were prepared. They were found to exhibit extremely high potency in the enzyme inhibition assay. These
Autor:
Joel R. Huff, James P. Guare, PaulL. Darke, William A. Schleif, I.-W. Chen, Jiunn H. Lin, Kari Vastag, B. Moon Kim, Drazen Ostovic, Emilio A. Emini, Joseph P. Vacca, Joan A. Zugay, Colleen M. Hanifin, Stuart R. Michelson, P. S. Anderson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:2273-2278
A new hydroxyethylamine class of inhibitors was designed combining features from our clinical candidate, L-735,524, along with small heterocyclic P 2 -ligands developed in these laboratories. Highly potent inhibitors possessing subnanomolar IC 50 's
Autor:
Jenny Wai, Paula M.D. Fitzgerald, Deborah J. Arford-Bickerstaff, Joel R. Huff, Paul L. Darke, James P. Guare, P. S. Anderson, Colleen M. Hanifin, M. Katharine Holloway, B. Moon Kim, Joseph P. Vacca, Joan A. Zugay
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:2199-2204
A new class of conformationally restricted HIV-1 protease inhibitors was designed based upon molecular modeling studies of known hydroxyethylamine (HEA) type inhibitors. The structure activity relationships for this series of compounds are discussed
Autor:
Arun K. Ghosh, Wayne J. Thompson, M. Katharine Holloway, Sean P. McKee, Tien T. Duong, Hee Yoon Lee, Peter M. Munson, Anthony M. Smith, Jenny M. Wai, Paul L. Darke, Joan A. Zugay, Emilio A. Emini, William A. Schleif, Joel R. Huff, Paul S. Anderson
Publikováno v:
Journal of Medicinal Chemistry. 36:2300-2310
A series of protease inhibitors bearing constrained unnatural amino acids at the P2-position and novel heterocycles at the P3-position of compound 1 (Ro 31-8959) were synthesized, and their in vitro enzyme inhibitory and antiviral activities were eva
Autor:
Jenny Wai, M. K. Holloway, Arun K. Ghosh, Paul L. Darke, Hee Yoon Lee, Joel R. Huff, P. S. Anderson, John E. Schwering, Wayne J. Thompson, Emilio A. Emini, William A. Schleif, Joan A. Zugay, P. M. Munson
Publikováno v:
ChemInform. 24
Publikováno v:
ChemInform. 24
The synthesis of a differentially protected dipeptide mimic 10 in enantiomerically pure form is described. The key step involves the epimerization of the C-2 center of the lactone 4, hydrolysis and protection of the resulting hydroxy acid, followed b
Autor:
M. K. Holloway, Paul L. Darke, A. M. Smith, P. S. Anderson, Joan A. Zugay, Hee Yoon Lee, Wayne J. Thompson, Emilio A. Emini, C. Culberson, S. P. Mckee, P. M. Munson, Joel R. Huff, William A. Schleif, T. T. Duong, Arun K. Ghosh
Publikováno v:
ChemInform. 25