Zobrazeno 1 - 10
of 32
pro vyhledávání: '"J. P. Vacca"'
Autor:
James Z. Deng, S. D. Lewis, P.M. Rabbat, Craig A. Coburn, Terry A. Lyle, J. P. Vacca, Bobby J. Lucas, Daniel R. McMasters, Julie A. Krueger, B. Strulovici, Youwei Yan, Peter D. Williams, Lawrence Kuo, Christopher S. Burgey
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:4411-4416
Thrombin-inhibitor X-ray crystal structures, in combination with the installation of binding elements optimized within the pyrazinone series of thrombin inhibitors, were utilized to transform a weak triazolopyrimidine lead into a series of potent oxa
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:
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
Autor:
E P Baskin, Adel M. Naylor-Olsen, C. M. Cooper, Appleby Sd, J. P. Vacca, K B Dancheck, Stephen J. Gardell, Elizabeth A. Lyle, William C. Lumma, I.-W. Chen, John T. Sisko, S. D. Lewis, Julie A. Krueger, R Woltmann, J.J. Lynch, Bobby J. Lucas, Thomas J. Tucker
Publikováno v:
Journal of Medicinal Chemistry. 40:3687-3693
As part of an effort to prepare efficacious and orally bioavailable analogs of the previously reported thrombin inhibitors 1a,b, we have synthesized a series of compounds that utilize 3,3-disubstituted propionic acid derivatives as P 3 ligands. By re
Autor:
E P Baskin, J.J. Lynch, Elizabeth A. Lyle, William C. Lumma, Thomas J. Tucker, Appleby Sd, K B Dancheck, I.-W. Chen, Bobby J. Lucas, S. D. Lewis, J. P. Vacca, Stephen J. Gardell, R Woltmann
Publikováno v:
Journal of Medicinal Chemistry. 40:1565-1569
In an effort to prepare orally bioavailable analogs of our previously reported thrombin inhibitor 1, we have synthesized a series of compounds that utilize the unique amino acid D-dicyclohexylalanine as a P3 ligand. The resulting compounds are extrem
Autor:
M K, Holloway, J M, Wai, T A, Halgren, P M, Fitzgerald, J P, Vacca, B D, Dorsey, R B, Levin, W J, Thompson, L J, Chen, S J, deSolms
Publikováno v:
Journal of Medicinal Chemistry. 38:305-317
We have observed a high correlation between the intermolecular interaction energy (E inter ) calculated for HIV-1 protease inhibitor complexes and the observed in vitro enzyme inhibition. A training set of 33 inhibitors containing modifications in th
Autor:
P.M.D. Fitzgerald, Joel R. Huff, Ken E. Starbuck, L.J. Chen, Hungate Randall W, Paul L. Darke, P. S. Anderson, M. K. Holloway, J. P. Vacca
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:499-504
The synsthesis and structure activity relationships of conformationally constrained analogs of the HIV-1 protease inhibitor L-685,434 are described. In addition, the X-ray crystal structure of a complex between L-700,497 and the HIV-1 protease is sho
Autor:
Emilio A. Emini, Drazen Ostovic, I-W. Chen, J. P. Guare, J. H. Lin, Joel R. Huff, Paul L. Darke, Kari Vastag, P. S. Anderson, Boyoung Kim, Colleen M. Hanifin, Stuart R. Michelson, William A. Schleif, J. P. Vacca, Joan A. Zugay
Publikováno v:
ChemInform. 26
Autor:
Emilio A. Emini, J. P. Guare, Joan A. Zugay, Paul L. Darke, Stuart R. Michelson, Joel R. Huff, P. S. Anderson, J. P. Vacca, William A. Schleif, J. H. Lin, I.-W. Chen, Boyoung Kim, Kari Vastag
Publikováno v:
ChemInform. 26
Autor:
Colleen M. Hanifin, Emilio A. Emini, Boyoung Kim, J. P. Vacca, Joel R. Huff, I.-W. Chen, J. H. Lin, P. S. Anderson, Joan A. Zugay, Paul L. Darke, Stuart R. Michelson, C. Blair Zartman, William A. Schleif, Kari Vastag
Publikováno v:
ChemInform. 27