Zobrazeno 1 - 5
of 5
pro vyhledávání: '"Dona L. Dyer"'
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:
Steven J. Gardell, S. Dale Lewis, Bobby J. Lucas, Sanderson Philip E, A. M. Mulichak, Joseph P. Vacca, Adel M. Naylor-Olsen, Dona L. Dyer, Joseph J. Lynch, Elizabeth A. Lyle
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 7:1497-1500
L-373,890, a highly selective and efficacious pyridinone acetamide thrombin inhibitor was designed using a combination of X-ray crystallography, molecular modeling and empirical structure optimization.
Autor:
Sanderson Philip E, B. J. Jun. Lucas, S. D. Lewis, Elizabeth A. Lyle, Dona L. Dyer, A. M. Mulichak, J. P. Vacca, Stephen J. Gardell, Adel M. Naylor-Olsen, J.J. Lynch
Publikováno v:
ChemInform. 28
Autor:
Bobby J. Lucas, Sanderson Philip E, S. Dale Lewis, Julie A. Krueger, Youwei Yan, Lawrence C. Kuo, Kellie J. Cutrona, Dona L. Dyer
Publikováno v:
ChemInform. 34
Use of a chlorophenoxyacetamide P1 group with a pyridinone acetamide P2/P3 gave an exceptionally potent thrombin inhibitor (K(i)=40 pM). Truncation of the molecule at the N-terminus gave unique, low nanomolar, non-covalent thrombin inhibitors which d
Autor:
Bobby J. Lucas, S. Dale Lewis, and Jules A. Shafer, Stephen J. Gardell, Maria T. Stranieri, Timothy R. Hare, Kellie J. Cutrona, Joseph J. Lynch, Dona L. Dyer, Adel M. Naylor-Olsen, Joseph P. Vacca, Sanderson Philip E, Colleen M. McDonough, Kari Vastag, Julie A. Krueger, Youwei Yan, Bruce D. Dorsey, C. M. Cooper, Terry A. Lyle, Zhongguo Chen, Elizabeth A. Lyle, I.-W. Chen, Jacquelynn J. Cook, Jiunn H. Lin
Publikováno v:
Journal of medicinal chemistry. 41(23)
We have addressed the key deficiency of noncovalent pyridinone acetamide thrombin inhibitor L-374,087 (1), namely, its modest half-lives in animals, by making a chemically stable 3-alkylaminopyrazinone bioisostere for its 3-sulfonylaminopyridinone co