Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Dalia R. Jakas"'
Autor:
William H. Miller, Frank Fan, Nicola G. Wallis, Mark A. Seefeld, Walter E. DeWolf, Martha S. Head, David J. Payne, Damien McDevitt, Jianzhong Huang, Terrance D. Moore, Dalia R. Jakas, Kenneth A. Newlander, Kang Yan, Stephen Rittenhouse, Shannon L. Reed
Publikováno v:
Antimicrobial Agents and Chemotherapy. 46:3343-3347
The MICs of triclosan for 31 clinical isolates of Staphylococcus aureus were 0.016 μg/ml (24 strains), 1 to 2 μg/ml (6 strains), and 0.25 μg/ml (1 strain). All the strains for which triclosan MICs were elevated (>0.016 μg/ml) showed three- to fiv
Autor:
David J. Rieman, William F. Huffaman, Kevin L. Salyers, Richard M. Keenan, Michael W. Lark, Janice A. Vasko-Moser, Thomas W. Ku, Maxine Gowen, Leonard M. Azzarano, Karl F. Erhard, Stephen T. Ross, Denise Zembryki, Bradbeer Jeremy N, Bondinell William E, Shing-Mei Hwang, William H. Miller, Kenneth A. Newlander, George B. Stroup, Beata Lechowska, Fred H. Drake, Keith W. Ward, Kyung O. Johanson, Brian R. Smith, Paula C. Adams, Ian E. James, R. Curtis Haltiwanger, Russell D. Cousins, Dalia R. Jakas, Sandra J. Hoffman
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:1807-1812
A new series of potent nonpeptide vitronectin receptor antagonists, based on a novel carbocyclic Gly-Asp mimetic, has been discovered. A representative of this series, SB 265123 (4), has 100% oral bioavailability in rats, and is orally active in vivo
Autor:
Richard M. Keenan, Steven T. Ross, M. Amparo Lago, S M Hwang, Eliot H. Ohlstein, Tian-Li Yue, David J. Rieman, Chet Kwon, Fadia E. Ali, Brian R. Smith, Lynne Vickery, Thomas T. Nguyen, Dalia R. Jakas, Russell D. Cousins, Calvert Louden, Jeffrey M. Stadel, Leon B. Hall, James Samanen, William H. Miller, Catherine C.K. Yuan, Dennis T. Takata
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:3171-3176
In the 3-oxo-1,4-benzodiazepine-2-acetic acid series of vitronectin receptor (alpha v beta 3) antagonists, a compound containing an imidazopyridine arginine mimetic was discovered which had sufficient potency and i.v. pharmacokinetics for demonstrati
Autor:
Thomas W. Ku, Dalia R. Jakas, William H. Miller, Valerie A. Reader, James F. Callahan, Catherine C.K. Yuan, Brian R. Smith, Dennis T. Takata, Raul R. Calvo, Thomas T. Nguyen, Bondinell William E, Fadia E. Ali, Russell D. Cousins, S M Hwang, Chet Kwon, Steven T. Ross, Irene N. Uzinskas, David J. Rieman, M. Amparo Lago, Richard M. Keenan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:3165-3170
In a 3-oxo-1,4-benzodiazepine-2-acetic acid series of vitronectin receptor (alpha v beta 3) antagonists containing a benzimidazole as a novel arginine mimetic, we examined the effects of benzimidazole modifications and amide substitutions on both act
Autor:
Philip L. Smith, Andrew J. Nichols, Tobias Oregon Yellin, Kenneth A. Newlander, Raul R. Calvo, James Samanen, Irene N. Uzinskas, Bondinell William E, Chao-Pin Lee, Michael W. Parker, Dalia R. Jakas
Publikováno v:
Advanced Drug Delivery Reviews. 23:133-142
A series of potent, high affinity GPIIb/IIIa antagonists were evaluated for intestinal permeability in vitro using rabbit intestinal strips mounted in the Ussing Chamber. In this series of compounds, structural modifications were found to impact inte
Autor:
Angela S. Wong, James F. Callahan, William H. Miller, Catherine C.K. Yuan, Raul R. Calvo, Janice A. Vasko-Moser, Thomas W. Ku, Richard E. Valocik, Dennis T. Takata, Richard M. Keenan, Drake S. Eggleston, Michael F. Parker, Southall Linda Sue, S M Hwang, Paul F. Koster, William F. Huffman, Tobias Oregon Yellin, Chet Kwon, Irene N. Uzinskas, Bondinell William E, Fadia E. Ali, Dalia R. Jakas, Andrew J. Nichols, James Samanen, R. Curtis Haltiwanger, Kenneth A. Newlander
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 6:2481-2486
In an investigation of the contribution of N-1 to the binding, antiaggregatory, and oral activity in 3-oxo-1,4-benzodiazepine-2-acetic acid based GPIIb/IIIa antagonists, a series of 2-benzazepine analogs, wherein N-1 of the 1,4-benzodiazepine nucleus
Autor:
Dulcie B. Schmidt, Israil Pendrak, Chambers Pamela Anne, Robert A. Daines, H. M. Sarau, Dalia R. Jakas, James J. Foley, William Dennis Kingsbury
Publikováno v:
ChemInform. 25
A series of trisubstituted pyridines have been prepared that exhibit in vitro leukotriene B4 (LTB4, 1) receptor antagonist activity. Previous disubstituted pyridines from these labs showed high affinity for the LTB4 receptor but demonstrated agonist
Autor:
Jeffrey C. Boehm, Dalia R. Jakas, Robert P. Hertzberg, Sidney M. Hecht, Gregory Gallagher, Randall K. Johnson, William Dennis Kingsbury, Leo F. Faucette, Francis L. McCabe, Mary Jo Caranfa, K. G. Holden
Publikováno v:
Journal of Medicinal Chemistry. 34:98-107
Water-soluble analogues of the antitumor alkaloid camptothecin (1) were prepared in which aminoalkyl groups were introduced into ring A or B. Most of the analogues were prepared by oxidation of camptothecin to 10-hydroxycamptothecin (2) followed by a
Autor:
Walter J. Burgess, Paul M. Keller, Nicola G. Wallis, Manley Peter J, William F. Huffman, Irene N. Uzinskas, Xiayang Qiu, David J. Payne, Kenneth A. Newlander, Stewart C. Pearson, Mark A. Seefeld, Brian J. Polizzi, Walter E. DeWolf, William H. Miller, Stephen Rittenhouse, Patricia A. Elkins, Martha S. Head, Cheryl A. Janson, Dalia R. Jakas, Terrance D. Moore
Publikováno v:
Journal of medicinal chemistry. 46(9)
Bacterial enoyl-ACP reductase (FabI) is responsible for catalyzing the final step of bacterial fatty acid biosynthesis and is an attractive target for the development of novel antibacterial agents. Previously we reported the development of FabI inhib
Autor:
Robert A. Daines, Israil Pendrak, James J. Foley, Don E. Griswold, Dulcie B. Schmidt, Lenox D. Martin, Dalia R. Jakas, M. N. Tzimas, Chambers Pamela Anne, Henry M. Sarau
Publikováno v:
Journal of Medicinal Chemistry. 36:2703-2705