Zobrazeno 1 - 10
of 30
pro vyhledávání: '"Susan Elizabeth Hagen"'
Autor:
J.V.N. Vara Prasad, Lou Chupak, Frederick E. Boyer, Michael Melnick, K. Gavardinas, M. Patterson, Susan Elizabeth Hagen, Qizhu Ding, Michael D. Huband, Karina Romero, Samarendra N. Maiti, Michael R. Dermyer, Takushi Kaneko, Wenhua Jiao, Xiujuan Wu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:5392-5397
We describe a novel class of benzocycloheptanone derived oxazolidinone antibacterial agents. The synthesis and antibacterial activities with structure variation is discussed.
The review by Domagala in 1994 represented one of the first attempts to simultaneously delineate the structure-activity relationships (SARs) of both activity and side effects providing some insights as to where the future of the quinolones might resi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::71e583c51d22a1ea09a3f29eb1215c09
https://doi.org/10.1128/9781555817817.ch1
https://doi.org/10.1128/9781555817817.ch1
Autor:
Bradley D. Tait, Susan Elizabeth Hagen, Michael Lovdahl, Eric Andrew Zeikus, Carolyn Nouhan, Joanne Brodfuehrer, Donald Hupe, Christopher Andrew Gajda, John M. Domagala, Greg Zeikus, Elizabeth A. Lunney, Steve Vanderroest, Alexander Pavlovsky, Andrej Urumov, James Saunders, Stephen J. Gracheck, Eric Wise, Tod P. Holler
Publikováno v:
Journal of Medicinal Chemistry. 44:2319-2332
Due largely to the emergence of multi-drug-resistant HIV strains, the development of new HIV protease inhibitors remains a high priority for the pharmaceutical industry. Toward this end, we previously identified a 4-hydroxy-5,6-dihydropyrone lead com
Autor:
Larry J. Markoski, Stephen J. Gracheck, Carolyn Nouhan, Peter J. Tummino, Steven VanderRoest, James Saunders, J. V. N. Vara Prasad, Krishna R. Iyer, Christopher Gajda, Fred E. Boyer, Donna Ferguson, Elizabeth A. Lunney, John M. Domagala, Bradley Dean Tait, Michael Sinz, Donald Hupe, Tod P. Holler, Susan Elizabeth Hagen, Edmund L. Ellsworth
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:2217-2222
Dihydropyran-2-one possessing a sulfamate moiety at the 4-position of the thiophenyl ring were designed to reach S 3 ′ pocket of the HIV protease. Synthetic routes for the preparation of thiotosylates possessing 3-(2- t -butyl-5-methyl-4-sulfamate)
Autor:
J. V. N. Vara Prasad, Donald Hupe, Elizabeth A. Lunney, John M. Domagala, Donna Ferguson, Greg Zeikus, Neil Graham, Peter J. Tummino, Susan Elizabeth Hagen, Caroline Nouhan, Tod P. Holler, Edmund L. Ellsworth
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:2019-2024
5,6-Dihydro-2H-pyran-2-ones are potent inhibitors of HIV-1 protease, which bind to the S1, S2, S1', and S2' pockets and have a unique binding mode with the catalytic aspartyl groups and the flap region of the enzyme. Efforts to explore 3-position het
Autor:
Peter J. Tummino, James Saunders, Stephen J. Gracheck, Bradley Dean Tait, J. V. N. Vara Prasad, Joanne I. Brodfuehrer, Christopher Andrew Gajda, Krishna R. Iyer, Tod P. Holler, Susan Elizabeth Hagen, Steven VanderRoest, Edmund L. Ellsworth, Fred E. Boyer, Carolyn Nouhan, Donna Ferguson, Larry James Markoski, Michael Sinz, Donald Hupe, Elizabeth A. Lunney, John M. Domagala
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:1481-1486
Dihydropyran-2-ones possessing amino and carboxamide functionalities on 3-SPh (2-tert-butyl, 5-methyl) ring were synthesized and evaluated for their antiviral activities. Both the enantiomers of inhibitor 15 were synthesized. The in vitro resistance
Autor:
Elizabeth A. Lunney, Frederick E. Boyer, J. V. N. Vara Prasad, Stephen J. Gracheck, Carolyn Nouhan, Edmund L. Ellsworth, Bradley Dean Tait, Donna Ferguson, Susan Elizabeth Hagen, Steven VanderRoest, Larry J. Markoski, James Saunders, Harriet W. Hamilton, B. A. Steinbaugh, Peter J. Tummino, John M. Domagala, Donald Hupe, Christopher Gajda
Publikováno v:
Journal of Medicinal Chemistry. 40:3707-3711
Autor:
John W. Erickson, Donald Hupe, Eric T. Baldwin, J. R. Rubin, and Sergei V. Gulnik, Christine Humblet, Susan Elizabeth Hagen, Christopher Gajda, Harriet W. Hamilton, Carolyn Nouhan, Beishan Liu, J. V. N. Vara Prasad, Neil Graham, Edmund L. Ellsworth, Peter J. Tummino, John M. Domagala, Alexander Pavlovsky, Donna Ferguson, Elizabeth A. Lunney, T. N. Bhat, Bradley Dean Tait, Stephen J. Gracheck
Publikováno v:
Journal of Medicinal Chemistry. 40:3781-3792
The 4-hydroxy-5,6-dihydropyrone template was utilized as a flexible scaffolding from which to build potent active site inhibitors of HIV protease. Dihydropyrone 1c (5,6-dihydro-4-hydroxy-6-phenyl-3-[(2-phenylethyl)thio]-2H-pyran-2-one) was modeled in
Autor:
Christopher Gajda, Bradley Dean Tait, Peter J. Tummino, Harriet W. Hamilton, Susan Elizabeth Hagen, Alexander Pavlovsky, Donna Ferguson, Elizabeth A. Lunney
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 6:719-724
Publications from our laboratories have recently described a series of 3-thioaryl substituted-4-hydroxy-pyrones1 as HIV protease inhibitors. The current work examines the analogous 5,6-dihydro-2H-pyran-2-ones with 6,6-substitutions focusing on the us
Autor:
Takeshi Nakamura, Wataru Watanabe, Hidetsura Cho, Eric C Nordby, Peter Craig Weber, Harriet W. Hamilton, Susan Elizabeth Hagen, Stefanie L Boulware, Gisele Nishiguchi, Stephen J. Gracheck, John D Domagala, Satoru Ikeda
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:2981-2983
A series of novel benzthiodiazepinones was studied as antiherpetic agents. Significant improvements in potency and therapeutic index in a viral replication assay were realized over the starting molecule. The role of stereospecific substitution on the