Zobrazeno 1 - 9
of 9
pro vyhledávání: '"Darian M. Bartkowski"'
Autor:
Laurie A. LeBrun, Mei Tsan, Yuefen Zhou, Frank Ruebsam, Darian M. Bartkowski, Alan X. Xiang, Ruhi Kamran, Lian-Sheng Li, Richard E. Showalter, Jingjing Zhao, Rupal Patel, Matthew Lardy, Maria V. Sergeeva, Stephen E. Webber, Amit M. Shah, David Archer Ellis, Zhongxiang Sun, Mcguire Helen, Julie Blazel, Leo Kirkovsky, Daniel A. Norris, Tran Chinh Viet, Charles R. Kissinger, Thomas G. Nolan, Peter S. Dragovich, Qing Han
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:4628-4632
4-(1,1-Dioxo-1,4-dihydro-1lambda(6)-benzo[1,4]thiazin-3-yl)-5-hydroxy-2H-pyridazin-3-one analogs were discovered as a novel class of inhibitors of HCV NS5B polymerase. Structure-based design led to the identification of compound 3a that displayed pot
Autor:
Tran Chinh Viet, Charles R. Kissinger, Daniel A. Norris, Ruhi Kamran, Amit M. Shah, Jingjing Zhao, Yuefen Zhou, Rupal Patel, Matthew Lardy, Darian M. Bartkowski, Richard E. Showalter, Stephen E. Webber, Laurie A. LeBrun, Mei Tsan, Douglas E. Murphy, Sun Hee Kim, Maria V. Sergeeva, Leo Kirkovsky, Martin T. Tran, Thomas G. Nolan, Qing Han, Frank Ruebsam, Lian-Sheng Li, Peter S. Dragovich
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:3616-3621
Pyrrolo[1,2-b]pyridazin-2-one analogs were discovered as a novel class of inhibitors of genotype 1 HCV NS5B polymerase. Structure-based design led to the discovery of compound 3 k, which displayed potent inhibitory activities in biochemical and repli
Autor:
Tran Chinh Viet, Benjamin K. Ayida, Peter S. Dragovich, Amit M. Shah, Huiying J. Hou, Peggy A. Thompson, Frank Ruebsam, Jingjing Zhao, Rupal Patel, Daniel A. Norris, Ruhi Kamran, Thomas G. Nolan, Stephen E. Webber, Qing Han, Charles R. Kissinger, Alan X. Xiang, Lian-Sheng Li, Darian M. Bartkowski, Jennifer Brooks, Julia Khandurina, Ellen Okamoto, Zhongxiang Sun, Mei Tsan, Laurie A. LeBrun, Mcguire Helen, Julie K. Blazel, Maria V. Sergeeva, Sun Hee Kim, Yuefen Zhou, Douglas E. Murphy, Richard E. Showalter, Leo Kirkovsky
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(22)
A novel series of non-nucleoside small molecules containing a tricyclic dihydropyridinone structural motif was identified as potent HCV NS5B polymerase inhibitors. Driven by structure-based design and building on our previous efforts in related serie
Autor:
Ruhi Kamran, Tran Chinh Viet, Laurie A. LeBrun, Alberto Gobbi, Jingjing Zhao, David Archer Ellis, Qiang Zhao, Julie Blazel, Rupal Patel, Matthew Lardy, Maria V. Sergeeva, Thomas G. Nolan, Qing Han, Stephen E. Webber, Amit M. Shah, Yuefen Zhou, Frank Ruebsam, Richard E. Showalter, Darian M. Bartkowski, Leo Kirkovsky, Alan X. Xiang, Lian-Sheng Li, Douglas E. Murphy, Mei Tsan, Mcguire Helen, Charles R. Kissinger, Daniel A. Norris
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(21)
The discovery of 5,5'- and 6,6'-dialkyl-5,6-dihydro-1H-pyridin-2-ones as potent inhibitors of the HCV RNA-dependent RNA polymerase (NS5B) is described. Several of these agents also display potent antiviral activity in cell culture experiments (EC50
Autor:
Stephen E. Webber, Maria V. Sergeeva, Amit M. Shah, Rupal Patel, Frank Ruebsam, Leo Kirkovsky, Darian M. Bartkowski, Charles R. Kissinger, Benjamin K. Ayida, Thomas G. Nolan, Ruhi Kamran, Richard E. Showalter, Daniel A. Norris, Mei Tsan, Zhongxiang Sun, Laurie A. LeBrun, Qiang Zhao, Yuefen Zhou
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(18)
Hexahydro-pyrrolo- and hexahydro-1H-pyrido[1,2-b]pyridazin-2-one analogs were discovered as a novel class of inhibitors of genotype 1 HCV NS5B polymerase. Among these, compound 4c displayed potent inhibitory activities in biochemical and replicon ass
Autor:
Leo Kirkovsky, Julie Blazel, Tran Chinh Viet, Darian M. Bartkowski, Mei Tsan, Martin T. Tran, Stephen E. Webber, Douglas E. Murphy, Richard E. Showalter, David Archer Ellis, Qiang Zhao, Benjamin K. Ayida, Frank Ruebsam, Alberto Gobbi, Amit M. Shah, Alan X. Xiang, Rupal Patel, Charles R. Kissinger, Yuefen Zhou, Thomas G. Nolan, Daniel A. Norris, Qing Han, Sun Hee Kim, Maria V. Sergeeva, Laurie A. LeBrun, Mcguire Helen
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(14)
A novel series of HCV NS5B polymerase inhibitors comprising 1,1-dioxoisothiazoles and benzo[b]thiophene-1,1-dioxides were designed, synthesized, and evaluated. SAR studies guided by structure-based design led to the identification of a number of pote
Autor:
Ellen Okamoto, Ruhi Kamran, Leo Kirkovsky, Darian M. Bartkowski, Alberto Gobbi, Jingjing Zhao, Rupal Patel, Lian-Sheng Li, Matthew Lardy, Peter S. Dragovich, Laurie A. LeBrun, Stephen E. Webber, Nebojsa Stankovic, Mei Tsan, Maria V. Sergeeva, Daniel A. Norris, Amit M. Shah, Thomas G. Nolan, Yuefen Zhou, Douglas E. Murphy, Thomas M. Bertolini, Zhongxiang Sun
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(11)
5-Hydroxy-3(2H)-pyridazinone derivatives were investigated as potent inhibitors of genotype 1 HCV NS5B polymerase focusing on the optimization of their drug metabolism and pharmacokinetics (DMPK) profiles. This investigation led to the discovery of p
Autor:
Jingjing Zhao, Frank Ruebsam, Rupal Patel, Douglas E. Murphy, Tran Chinh Viet, Stephen E. Webber, Charles R. Kissinger, Nebojsa Stankovic, Lian-Sheng Li, Darian M. Bartkowski, Richard E. Showalter, Qiang Zhao, Mei Tsan, Benjamin K. Ayida, Zhongxiang Sun, Ruhi Kamran, Leo Kirkovsky, Peter S. Dragovich, Jennifer Brooks, Amit M. Shah, Laurie A. LeBrun, Maria V. Sergeeva, Thomas M. Bertolini, Thomas G. Nolan, Daniel A. Norris, Yuefen Zhou
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(11)
5-Hydroxy-3(2H)-pyridazinone derivatives were investigated as inhibitors of genotype 1 HCV NS5B polymerase. Lead optimization led to the discovery of compound 3a, which displayed potent inhibitory activities in biochemical and replicon assays [IC(50)
Autor:
Stephen E. Webber, Virginia N. Banh, Erik J. Rueden, Wei Li, Gregory J. Haley, Darian M. Bartkowski, Clark David Louis, Tingmin Wang, John S Ng, Mark R Herbert, Bradley M. Kerr, Leonid I Kirkovsky, Joseph R. Lennox, Alan X. Xiang, Averett Devron R, Simon P. Fletcher, Kevin R. Steffy, Lisa A Bauman
Publikováno v:
Nucleosides, nucleotidesnucleic acids. 26(6-7)
ANA975, a 5-amino-3-beta -D-ribofuranosyl-3H-thiazolo[4,5-d]pyrimidin-2-one derivative, was synthesized in the search of an oral prodrug of isatoribine, a small molecule toll-like receptor 7 (TLR-7) agonist. Several strategies were studied to enable