Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Trelia J. Craft"'
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1f7308733752c4e2e7235ca66a8d4df0
https://doi.org/10.1016/j.bmcl.2007.09.105
https://doi.org/10.1016/j.bmcl.2007.09.105
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9a61a45d3dd680208b1edccc60cf9e75
https://doi.org/10.1016/j.bmcl.2007.08.051
https://doi.org/10.1016/j.bmcl.2007.08.051
Autor:
Linebarger Jh, Michael Robert Wiley, Leonard C. Weir, Trelia J. Craft, Goodson T, Donetta S. Gifford-Moore, Kyle Ja, Jason Scott Sawyer, Valentine J. Klimkowski, David K. Herron, Anne Louise Tebbe, Smith Gf, Douglas W. Beight, Ying Kwong Yee, Jennifer M. Tinsley, Richard D. Towner
Publikováno v:
Journal of Medicinal Chemistry. 43:873-882
Reversal of the A-ring amide link in 1,2-dibenzamidobenzene 1 (fXa K(ass) = 0.81 x 10(6) L/mol) led to a series of human factor Xa (hfXa) inhibitors based on N(2)-aroylanthranilamide 4. Expansion of the SAR around 4 showed that only small planar subs
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8a3d1c67ef532a58d8c77eb9f6859273
https://doi.org/10.1021/jm990327e
https://doi.org/10.1021/jm990327e
Autor:
Robert Theodore Shuman, Nickolay Y. Chirgadze, William J. Coffman, David K. Clawson, Michael Robert Wiley, Leonard C. Weir, Gerald F. Smith, Aaron Leigh Schacht, Donnetta Gifford-Moore, Noel D. Jones, Jennifer L. Olkowski, Trelia J. Craft
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 5:2529-2534
We have prepared a series of tripeptide arginine aldehydes in which the P2 proline has been replaced with a variety of N -substituted glycines. The effects of these modifications on thrombin inhibitory potency and serine protease selectivity were eva
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ff7500a2d925f48d60a556d54d7eb094
https://doi.org/10.1016/0960-894x(95)00444-x
https://doi.org/10.1016/0960-894x(95)00444-x
Publikováno v:
Fibrinolysis. 7:264-274
We report the pharmacodynamic and pharmacokinetic evaluation of modified tissue plasminogen activator, LY210825, in the conscious dog upon intravenous (i.v.), subcutaneous (s.c.), and intramuscular (i.m.) injection of the single chain form of the thr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::893f64b313a248b5055e4cad84d81240
https://doi.org/10.1016/0268-9499(93)90135-i
https://doi.org/10.1016/0268-9499(93)90135-i
Autor:
Marcia L. Kellam, William J. Coffman, Gerald F. Smith, Michael L. Denney, Daniel Jon Sall, Trelia J. Craft, Dennis R. Berry, Donetta S. Gifford-Moore
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 2:1025-1028
Methyl 3-(2-methyl-1-oxopropoxy)[1]benzothieno[3,2-b]furan-2-carboxylate (LY806303; 1) has been characterized as a novel, potent and selective inhibitor thrombin.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a5cdaf16bce1671d27fdb130370c3c45
https://doi.org/10.1016/s0960-894x(00)80611-3
https://doi.org/10.1016/s0960-894x(00)80611-3
Autor:
Philip J. Burck, J F Quay, J L Bobbitt, Trelia J. Craft, Charles V. Jackson, V G Crowe, J L Sundboom, B W Grinnell, Gerald F. Smith
Publikováno v:
Circulation. 82:930-940
LY210825, a recombinant tissue-type plasminogen activator (rt-PA), which contains the kringle-2 and serine protease functional domains of native tissue-type plasminogen activator, was previously produced by site-directed mutagenesis in a Syrian hamst
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1431006b7bd026f80a6ddba01d5a6f0f
https://doi.org/10.1161/01.cir.82.3.930
https://doi.org/10.1161/01.cir.82.3.930
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6e3be392c7c1b54698da386ef5b5fe5e
https://pubmed.ncbi.nlm.nih.gov/17624775
https://pubmed.ncbi.nlm.nih.gov/17624775
Autor:
Kim E. Garbison, Trelia J. Craft, Mark W. Farmen, Philip W. Iversen, Gerald F. Smith, Neil W. DeLapp, Jeffrey K. Smallwood, Brian J. Eastwood
Publikováno v:
Journal of biomolecular screening. 11(3)
The authors show by illustration that procedures used to validate the reliability of single-concentration high-throughput screens such as the signal window and Z' factor do not ensure sufficient reliability in potency estimates from concentration res
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0f79aeb0cdbbfde0960a0bc4b47f0af3
https://pubmed.ncbi.nlm.nih.gov/16490778
https://pubmed.ncbi.nlm.nih.gov/16490778
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::82de30aceb6e4954485e45bc239ae835
https://pubmed.ncbi.nlm.nih.gov/16140530
https://pubmed.ncbi.nlm.nih.gov/16140530