Zobrazeno 1 - 6
of 6
pro vyhledávání: '"Jeffry Bernard Franciskovich"'
Autor:
Gerald F. Smith, Wayne W. Weber, John Walter Nr Macclesfield Liebeschuetz, Philip Sipes, Jeffry Bernard Franciskovich, Richard D. Towner, John Joseph Masters, Donetta S. Gifford-Moore, Trelia J. Craft, Ronald S. Foster, Jeffrey K. Smallwood, Michael L. Chouinard, Lea M. Johnson, Larry L. Froelich, Stephen C. Young, David W. Snyder, Marcia K. Chastain, Valentine J. Klimkowski, Christopher W. Murray
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:6910-6913
Several P4 domain derivatives of the general d-phenylglycinamide-based scaffold (2) were synthesized and evaluated for their ability to bind to the serine protease factor Xa. Some of the more potent compounds were evaluated for their anticoagulant ef
Autor:
Scott Martin Sheehan, Nikolay Y. Chirgadze, Gerald F. Smith, Jolie Anne Bastian, Michael Robert Wiley, Trelia J. Craft, Daniel Jon Sall, Jeffrey K. Smallwood, Jothirajah Marimuthu, John Walter Nr Macclesfield Liebeschuetz, Marcia K. Chastain, Philip Sipes, Jeffry Bernard Franciskovich, Brian Morgan Watson, Ronald S. Foster, Valentine J. Klimkowski
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:5801-5805
Analogs to a series of D-phenylglycinamide-derived factor Xa inhibitors were discovered. It was found that the S4 amide linkage can be replaced with an ether linkage to reduce the peptide character of the molecules and that this substitution leads to
Autor:
Larry L. Froelich, Andrew Michael Ratz, Leonard C. Weir, Anne Louise Tebbe, Gerald F. Smith, Valentine J. Klimkowski, John Joseph Masters, David K. Herron, John A. Buben, Kyle Ja, Angela Lynn Marquart, Jeffry Bernard Franciskovich, Richard D. Towner, Michael Robert Wiley, Philip Parker Waid, Jennifer M. Tinsley, Trelia J. Craft, Ying K. Yee, Theodore Goodson, David Mendel, Sajan Joseph
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(17)
SAR about the B-ring of a series of N 2 -aroyl anthranilamide factor Xa (fXa) inhibitors is described. B-ring o -aminoalkylether and B-ring p -amine probes of the S1′ and S4 sites, respectively, afforded picomolar fXa inhibitors that performed well
Autor:
Trelia J. Craft, Valentine J. Klimkowski, Jeffrey K. Smallwood, Jennifer M. Tinsley, Jeffry Bernard Franciskovich, Larry L. Froelich, Donetta S. Gifford-Moore, Michael Robert Wiley, T. C. Smith, Leonard C. Weir, Richard R. Towner, John Joseph Masters, Gerald F. Smith
Publikováno v:
Bioorganicmedicinal chemistry letters. 15(21)
Several non-amidino S1 derivatives of the 1,2-diaminobenzene-based scaffold (4) were synthesized and evaluated for their ability to bind to the active site and inhibit the human protease factor Xa. A subset of these compounds were also evaluated for
Autor:
Richard D. Towner, Robert Theodore Shuman, David K. Herron, Jeffry Bernard Franciskovich, John Joseph Masters, Michael Robert Wiley, Kenneth D. Kurz, T. C. Smith, Andrew Michael Ratz, and Alex Wilson, Jack B. Campbell, Charles S. Campbell, Valentine J. Klimkowski, Larry L. Froelich, Donetta S. Gifford-Moore, Ying K. Yee, James T. Metz, Lynne A. Hay, Jennifer M. Tinsley, Trelia J. Craft, Gerald F. Smith
Publikováno v:
Journal of medicinal chemistry. 43(11)
Autor:
Brian J. Eastwood, Guy Milot, Anne Louise Tebbe, Andrew Michael Ratz, Douglas W. Beight, Michael Robert Wiley, Ying Kwong Yee, Steven E. Hall, Leonard C. Weir, Jason Scott Sawyer, Jennifer M. Tinsley, Kyle Ja, Jeffry Bernard Franciskovich, Joseph John Masters, David Mendel, Richard D. Towner, Valentine J. Klimkowski, Smith Gf, Trelia J. Craft, James H. Wikel, David K. Herron, Donetta S. Gifford-Moore, Goodson T
Publikováno v:
Journal of medicinal chemistry. 43(5)
High-throughput screening of a combinatorial library of diamidophenols yielded lead compounds with the ability to inhibit human factor Xa (fXa) at micromolar concentrations (e.g. compound 4, fXa apparent K(ass) = 0.64 x 10(6) L/mol). SAR studies in t