Zobrazeno 1 - 10
of 11
pro vyhledávání: '"Christina L. Newton"'
Autor:
S. D. Lewis, Youwei Yan, Richard C.A. Isaacs, M. G. Solinsky, Lawrence Kuo, Julie A. Krueger, Bobby J. Lucas, Kellie J. Cutrona, Elizabeth A. Lyle, Adel M. Naylor-Olsen, Christina L. Newton, Daniel R. McMasters, J.J. Lynch
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:2062-2066
Guided by X-ray crystallography of thrombin-inhibitor complexes and molecular modeling, alkylation of the N1 nitrogen of the imidazole P1 ligand of the pyridinoneacetamide thrombin inhibitor 1 with various acetamide moieties furnished inhibitors with
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::da1f51337db1ab8622bb97fcfc58a61e
https://doi.org/10.1016/j.bmcl.2008.01.098
https://doi.org/10.1016/j.bmcl.2008.01.098
Autor:
Robinson Kyle A, Terry A. Lyle, Audrey A. Wallace, Christina L. Newton, Zhongguo Chen, James Z. Deng, Cynthia Miller-Stein, Bobby J. Lucas, Daniel R. McMasters, Janetta M. Pellicore, Harold G. Selnick, Joseph J. Lynch, Rebecca B. White, Lawrence Kuo, Julie A. Krueger, Christopher S. Burgey, Bradley K. Wong, Youwei Yan, Joseph P. Vacca, S. Dale Lewis, Jules A. Shafer, Stephen J. Gardell, Philippe G. Nantermet
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:2771-2775
In this study, we have demonstrated that the critical hydrogen bonding motif of the established 3-aminopyrazinone thrombin inhibitors can be effectively mimicked by a 2-aminopyridine N-oxide. As this peptidomimetic core is more resistant toward oxida
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3aef44dc180ef4edd6ed211a2de81f5d
https://doi.org/10.1016/j.bmcl.2005.03.110
https://doi.org/10.1016/j.bmcl.2005.03.110
Autor:
Philippe G. Nantermet, Harold G. Selnick, Youwei Yan, Bobby J. Lucas, Janetta M. Pellicore, Joseph P. Vacca, Julie A. Krueger, James C. Barrow, Christina L. Newton, S. Dale Lewis, Mary Beth Young, Lawrence C. Kuo, Daniel R. McMasters
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:2781-2784
A series of potent and selective proline- and pyrazinone-based macrocyclic thrombin inhibitors is described. Detailed SAR studies led to the incorporation of specific functional groups in the tether that enhanced functional activity against thrombin
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5f65a7a74a795c0575dc5998cddbcb3d
https://doi.org/10.1016/s0960-894x(03)00506-7
https://doi.org/10.1016/s0960-894x(03)00506-7
Autor:
Colleen M. McDonough, Emilio A. Emini, Bruce D. Dorsey, Paul L. Darke, Mark Stahlhut, William A. Schleif, Stuart R. Michelson, I-W. Chen, David B. Olsen, Carrie A. Rutkowski, Joseph P. Vacca, Stacey L. McDaniel, Joan Zugay-Murphy, Rhonda B. Levin, Jiunn H. Lin, M. Katharine Holloway, Lawrence C. Kuo, Jacob M. Hoffman, Christina L. Newton, and Joel R. Huff
Publikováno v:
Journal of Medicinal Chemistry. 43:3386-3399
Recent results from human clinical trials have established the critical role of HIV protease inhibitors in the treatment of acquired immune-deficiency syndrome (AIDS). However, the emergence of viral resistance, demanding treatment protocols, and adv
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1b883bd7828f12a025a3e8342b3125a8
https://doi.org/10.1021/jm9903848
https://doi.org/10.1021/jm9903848
Autor:
S. Dale Lewis, Kellie J. Cutrona, Maria T. Michener, Richard C.A. Isaacs, Elizabeth A. Lyle, Jacquelynn J. Cook, Christina L. Newton, Joseph J. Lynch, Colleen M. McDonough, Bobby J. Lucas, Bruce D. Dorsey, Julie A. Krueger, Rebecca B. White, Cynthia Miller-Stein, Swati P. Mercer, Audrey A. Wallace, Bradley K. Wong
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(5)
Although the S3 pocket of the thrombin active site is lined with lipophilic amino acid residues, the accommodation of polarity within the lipophilic P3 moiety of small molecule inhibitors is possible provided that the polar functionality is capable o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d0d6e57a55faa9972d6dee60338cae4f
https://pubmed.ncbi.nlm.nih.gov/21295466
https://pubmed.ncbi.nlm.nih.gov/21295466
Autor:
Maria T. Michener, Payne Linda S, K.J. Stauffer, S. Dale Lewis, Kellie J. Cutrona, Julie A. Krueger, Peter D. Williams, Bobby J. Lucas, Richard C.A. Isaacs, Joseph J. Lynch, Adel M. Naylor-Olsen, Daniel R. McMasters, Swati P. Mercer, Audrey A. Wallace, Elizabeth A. Lyle, Jacquelynn J. Cook, Christina L. Newton
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(5)
A novel 1,3,5-trisubstituted benzamide thrombin inhibitor template was designed via hybridization of a known aminopyridinoneacetamide and a known 1,3,5-trisubstituted phenyl ether. Optimization of this lead afforded a novel potent series of biaryl 1,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ff4791a3e113986b66f2e65f7a28883b
https://pubmed.ncbi.nlm.nih.gov/21295467
https://pubmed.ncbi.nlm.nih.gov/21295467
Autor:
S. Dale Lewis, Adel M. Naylor-Olsen, Julie A. Krueger, Richard C.A. Isaacs, Mark G. Solinsky, Christina L. Newton, Kellie J. Cutrona, Bobby J. Lucas
Publikováno v:
Bioorganicmedicinal chemistry letters. 16(2)
Despite their relatively weak basicity, simple azoles, specifically imidazoles and aminothiazoles, can function as potent surrogates for the more basic amines (e.g., alkyl amines, amidines, guanidines, etc.) which are most often employed as the P1 li
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::af8e469e2155418440af8bcabf0ead4a
https://pubmed.ncbi.nlm.nih.gov/16257203
https://pubmed.ncbi.nlm.nih.gov/16257203
Autor:
Rominder Singh, K.J. Stauffer, S. Dale Lewis, Marie A. Holahan, Daniel R. McMasters, Youwei Yan, Harold G. Selnick, Rebecca B. White, Matthew M. Zrada, Peter D. Williams, Audrey A. Wallace, Joseph J. Lynch, Maria Stranieri-Michener, Beth Pietrak, Cynthia Miller-Stein, Bradley K. Wong, Yvonne M. Leonard, Julie A. Krueger, G. R. Sitko, Philippe G. Nantermet, Bobby J. Lucas, Jacquelyn J. Cook, Carl F. Homnick, Elizabeth A. Lyle, Christina L. Newton
Publikováno v:
Journal of medicinal chemistry. 48(7)
Optimization of a previously reported thrombin inhibitor, 9-hydroxy-9-fluorenylcarbonyl-l-prolyl-trans-4-aminocyclohexylmethylamide (1), by replacing the aminocyclohexyl P1 group provided a new lead structure, 9-hydroxy-9-fluorenylcarbonyl-l-prolyl-2
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cd3aca135659209619e69ed0f3ccd38b
https://pubmed.ncbi.nlm.nih.gov/15801822
https://pubmed.ncbi.nlm.nih.gov/15801822
Autor:
James C. Barrow, Kenneth E. Rittle, Lawrence C. Kuo, Audrey A. Wallace, Bobby J. Lucas, George F. Lundell, Beth Pietrak, Harold G. Selnick, Rebecca B. White, S. Dale Lewis, Franklin C. Clayton, Christina L. Newton, Youwei Yan, Janetta M. Pellicore, Daniel R. McMasters, Peter D. Williams, Philippe G. Nantermet, Kenneth J. Stauffer, Bradley K. Wong, Cynthia Miller-Stein, Kristen L. Glass, Julie A. Krueger, Mary Beth Young, Jacquelynn J. Cook, Joseph P. Vacca, Dennis L. Bohn
Publikováno v:
Journal of medicinal chemistry. 47(12)
In an effort to discover potent, clinically useful thrombin inhibitors, a rapid analogue synthetic approach was used to explore the P(1) region. Various benzylamines were coupled to a pyridine/pyrazinone P(2)-P(3) template. One compound with an o-thi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9ebdb36312ce61d537b8ef9c3036ccbb
https://pubmed.ncbi.nlm.nih.gov/15163182
https://pubmed.ncbi.nlm.nih.gov/15163182
Autor:
Harold G. Selnick, Lawrence C. Kuo, Kellie J. Cutrona, Bobby J. Lucas, Kristen L. Glass, Joseph P. Vacca, Youwei Yan, S. Dale Lewis, Christina L. Newton, Daniel R. McMasters, Philippe G. Nantermet, Kenneth E. Rittle, William M. Sanders, Julie A. Krueger, Matthew M. Morrissette, James C. Barrow
Publikováno v:
Bioorganicmedicinal chemistry letters. 13(20)
Thrombin inhibitors incorporating o -aminoalkylbenzylamides in the P1 position were designed, synthesized and found to have enhanced potency and selectivity in several different structural classes. X-ray crystallographic analysis of compound 24 bound
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8b3803c7c869e32f8704fe15aecff321
https://pubmed.ncbi.nlm.nih.gov/14505652
https://pubmed.ncbi.nlm.nih.gov/14505652