Zobrazeno 1 - 10
of 19
pro vyhledávání: '"Bradley Dean Tait"'
Autor:
Bradley Dean Tait, H. William Tedford, Chad A. Finkenbinder, Gary L. Benzon, Bruce A. Steinbaugh, Whitney Smith, Anna Tempczyk-Russell, Lin Bao, Robert M. Kennedy
Publikováno v:
Pesticide Biochemistry and Physiology. 106:124-140
Previously, scanning mutagenesis studies of the insecticidal peptide omega-hexatoxin-Hv1a identified a set of structural features used by the omega-hexatoxin-1 family to modulate insect calcium channels. These structural features were re-purposed as
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:
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
Publikováno v:
Pharmaceutical Research. 15:1401-1406
Purpose. The feasibility of using hydrophobicity measurements as screens for intracellular availability in T-cells or intestinal permeability in Caco-2 cells was examined.
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:
N. Suman-Chauhan, Louise Webdale, Bharat K. Trivedi, Terri S. Purchase, Bruce D. Roth, Bradley Dean Tait, Michael W. Wilson, C.E. Augelli-Szafran
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:2009-2014
Due to the interesting pharmacological activity observed for CI-988, a potent and selective CCK-B receptor antagonist, we have continued to study the SAR of this antagonist. This particular study examines the importance of the indole moiety for bindi
Autor:
Alan Daugherty, Kathryn Welch, Richard D. Dyer, Joseph A. Cornicelli, Thomas M.A. Bocan, Sandra M. Sendobry, Bharat K. Trivedi, Steven J. Feinmark, Norman L. Colbry, Bradley Dean Tait
Publikováno v:
British Journal of Pharmacology. 120:1199-1206
1. 15-Lipoxygenase (15-LO) has been implicated in the pathogenesis of atherosclerosis because of its localization in lesions and the many biological activities exhibited by its products. To provide further evidence for a role of 15-LO, the effects of
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:
Elizabeth A. Lunney, Donna Ferguson, Edmund L. Ellsworth, Bradley Dean Tait, Donald Hupe, Christopher Gajda, John M. Domagala, Peter J. Tummino
Publikováno v:
Journal of Molecular Recognition. 9:139-142
New templates were designed and prepared which straddle the active site of HIV-1 protease. These templates were designed to be "flexible scaffolds' upon which substituents could be appended to fill the pockets of HIV protease. The new templates prepa