Zobrazeno 1 - 10
of 29
pro vyhledávání: '"Adel M. Naylor-Olsen"'
Autor:
Wenye Sun, Zhenmin He, Adel M. Naylor-Olsen, Deming Xu, Joseph P. Vacca, Leanne Bedard, Ashlee M. Earl, Christina Scherer, Abigail L. Manson, Maurice D. Lee, Diane M Rush, Mark E. Fitzgerald, Mingliang Zhang, Huisheng Xu, Michelle Palmer, Joshua A. Bittker, Michael Foley, Jean-Charles Marie, Jeremy R. Duvall, Giovanni Muncipinto
Publikováno v:
ACS Infectious Diseases. 3:349-359
In 2013, the Centers for Disease Control highlighted Clostridium difficile as an urgent threat for antibiotic-resistant infections, in part due to the emergence of highly virulent fluoroquinolone-resistant strains. Limited therapeutic options current
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
Autor:
Thomayant Prueksaritanont, Kara Merkle, John H. Hutchinson, Carmen Fernandez-Metzler, Mark E. Duggan, Audrey A. Wallace, Sevgi B. Rodan, Gary L. Stump, Hunt Cecilia, Michael J. Breslin, Adel M. Naylor-Olsen, Wasyl Halczenko, Chih-Tai Leu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:1809-1812
Two novel series of small-molecule RGD mimetics containing either a substituted pyridone or pyrazinone central constraint were prepared. Modification of the β-alanine 3-substituent produced compounds that are potent and selective α v β 3 antagonis
Autor:
Dennis L. Bohn, Sanderson Philip E, Bobby J. Lucas, Adel M. Naylor-Olsen, Julie A. Krueger, Elizabeth A. Lyle, Franklin C. Clayton, Youwei Yan, S. Dale Lewis, Denise J. Bickel, Denice C. Welsh, Kellie J. Cutrona, Audrey A. Wallace, Kelly L. Savage
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:1441-1444
We describe a series of highly potent and efficacious thrombin inhibitors based on a 3-amino-4-sulfonylpyridinone acetamide template. The functionally dense sulfonyl group stabilizes the aminopyridinone, conformationally constrains the 4-substituent,
Autor:
Adel M. Naylor-Olsen, Jacquelynn J. Cook, Robert J. Meissner, Amy E. Zartman, William F. Hoffman, Robert J. Gould, Guixiang Zhang, George D. Hartman, Joan D. Glass, R. J. Lynch, Mark E. Duggan, James J. Perkins
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:863-868
A new series of potent, linearly-minimized, orally active, selective GPIIb/IIIa inhibitors is identified. Thus 15 (L-750,034) achieves interaction via a constrained, non-turned conformation that maintains the proper distance between its charged termi
Autor:
Adel M. Naylor-Olsen, John T. Sisko, K.J. Stauffer, Elizabeth P. Baskin, Stephen F. Brady, C. M. Cooper, Maria T. Stranieri, Julie A. Krueger, K B Dancheck, Thomas J. Tucker, Elizabeth A. Lyle, J.J. Lynch, I.-W. Chen, Bobby J. Lucas, Jacquelynn J. Cook, William C. Lumma, S. D. Lewis, J. P. Vacca, Stephen J. Gardell, Marie A. Holahan, Youwei Yan
Publikováno v:
Journal of Medicinal Chemistry. 41:3210-3219
As part of an ongoing effort to prepare therapeutically useful orally active thrombin inhibitors, we have synthesized a series of compounds that utilize nonbasic groups in the P1 position. The work is based on our previously reported lead structure,
Autor:
Jules A. Shafer, Charles N. Habecker, Joseph P. Vacca, William M. Sanders, Thomas J. Tucker, Zhonguo Chen, A. M. Mulichak, S. Dale Lewis, Gerald S. Ponticello, Adel M. Naylor-Olsen, Brian T. Phillips
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:1697-1702
A novel, nonpeptidyl thrombin inhibitor, L-636,619 (1), was identified via topological similarity searching over the Merck Corporate Sample Database. X-ray crystallographic studies determined the geometry for ligand binding to the enzyme. Chemical mo
Autor:
John J. Baldwin, S. Dale Lewis, D. Dumas, Adel M. Naylor-Olsen, Gérard Leclerc, Murcko Mark A
Publikováno v:
European Journal of Medicinal Chemistry. 33:471-488
Thrombin plays a central role in thrombosis. Because of the medical need for novel antithrombotic drugs, a search for structurally novel thrombin inhibitors was undertaken. In the absence of a crystal structure, a class was designed based on a modeli
Autor:
S. Dale Lewis, Elizabeth A. Lyle, I.-W. Chen, Julie A. Krueger, Jacquelynn J. Cook, Zhongguo Chen, Jiunn H. Lin, Joseph P. Vacca, Bruce D. Dorsey, Adel M. Naylor-Olsen, Jules A. Shafer, Joseph J. Lynch, Kellie J. Cutrona, Bobby J. Lucas, Colleen M. McDonough, Dona L. Dyer, Maria T. Stranieri, Sanderson Philip E, Kari Vastag, Stephen J. Gardell
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:817-822
Replacement of the amidinopiperidine P1 group of 3-benzylsulfonylamino-6-methyl-2-pyridinone acetamide thrombin inhibitor L-373,890 (2) with a mildly basic 5-linked 2-amino-6-methylpyridine results in an equipotent compound L-374,087 (5, Ki = 0.5 nM)
Autor:
Kari Vastag, Ramjit Hg, J.J. Lynch, Stephen F. Brady, J. H. Lin, Marie A. Holahan, J. P. Vacca, Maria T. Stranieri, Adel M. Naylor-Olsen, Stephen J. Gardell, Elizabeth A. Lyle, I.-W. Chen, S. D. Lewis, William C. Lumma, Jacquelynn J. Cook, Smith Gm, Bobby J. Lucas, Appleby Sd, K.J. Stauffer
Publikováno v:
Journal of Medicinal Chemistry. 41:401-406
Early studies in these laboratories of peptidomimetic structures containing a basic P1 moiety led to the highly potent and selective thrombin inhibitors 2 (Ki = 5.0 nM) and 3 (Ki = 0.1 nM). However, neither attains significant blood levels upon oral