Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Dashyant Dhanak"'
Autor:
Nannan Liu, Michael N. Zimmerman, Richard M. Keenan, Victor K. Johnston, Deping Chai, Rosanna Tedesco, Duke M. Fitch, Juili Lin-Goerke, Kenneth Wiggall, Antony N. Shaw, Nestor O. Concha, Ramesh Bambal, Michael G. Darcy, Robert T. Sarisky, Dashyant Dhanak, Kevin J. Duffy, Adam T. Gates
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:4350-4353
The synthesis and optimisation of HCV NS5B polymerase inhibitors with improved potency versus the existing compound 1 is described. Substitution in the benzothiadiazine portion of the molecule, furnishing improvement in potency in the high protein Re
Autor:
Thomas J. Carr, Dashyant Dhanak, David Haigh, George Burton, Victor K. Johnson, Pia Thommes, Glenn A. Hofmann, Robert T. Sarisky, Martin John Slater, Juili Lin-Goerke, Thomas W. Ku, Nigel R. Parry, Terry Kiesow
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:1930-1933
The SAR development is described for a series of N -acyl pyrrolidine inhibitors of the Hepatitis C virus RNA-dependent RNA polymerase, NS5B, from tractable Δ21 enzyme inhibitors to an example with antiviral activity in a cellular assay (HCV replicon
Autor:
Chao Han, Warren W. Gerhardt, Dashyant Dhanak, Kevin J. Duffy, Nestor O. Concha, Adam T. Gates, Richard M. Keenan, Victor K. Johnston, Glenn A. Hofmann, Duke M. Fitch, Nannan Liu, Kenneth Wiggall, Antony N. Shaw, Dina L. Halegoua, Robert T. Sarisky, Michael N. Zimmerman, Ramesh Bambal, Michael G. Darcy, Arun C. Kaura, Juili Lin-Goerke, Deping Chai, Rosanna Tedesco
Publikováno v:
Journal of Medicinal Chemistry. 49:971-983
Recently, we disclosed a new class of HCV polymerase inhibitors discovered through high-throughput screening (HTS) of the GlaxoSmithKline proprietary compound collection. This interesting class of 3-(1,1-dioxo-2H-1,2,4-benzothiadiazin-3-yl)-4-hydroxy
Autor:
Breen Ann L, Lance Ridgers, David G. Tew, Dashyant Dhanak, Arun C. Kaura, Paddy Lavery, George Burton, Andrew West, Dinubhai H. Shah, Richard M. Keenan, Michael G. Darcy
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:3677-3682
A novel class of CMV protease inhibitors based on a benzothiopyran-S,S-dioxide nucleus has been discovered. Enzyme kinetic data supports a reversible mode of inhibition for a representative member of this class, 2-(3-pyridyl-N-oxide)benzothiopyran-4-
Autor:
Rosanna Tedesco, Duke M. Fitch, Robert T. Sarisky, Antony N. Shaw, Michael N. Zimmerman, Kevin J. Duffy, Michael G. Darcy, Dashyant Dhanak, Juili Lin-Goerke, Richard M. Keenan, Adam T. Gates, Victor K. Johnston, Deping Chai, Kenneth Wiggall, Klára Valkó
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(15)
Modification of the benzo rings of 3-(1,1-dioxo-2H-(1,2,4)-benzothiadiazin-3-yl)-4-hydroxy-2(1H)-quinolinones into heteroaromatic systems was investigated to enhance physicochemical properties and potency profile of this class of inhibitors. The synt
Autor:
Robert T. Sarisky, Juili Lin-Goerke, Thomas W. Ku, Glenn A. Hofmann, Richard M. Keenan, Terry Kiesow, Thomas J. Carr, Audrey Baker, George Burton, David L. Earnshaw, Dashyant Dhanak
Publikováno v:
Bioorganicmedicinal chemistry letters. 15(6)
HTS of the compound collection for inhibition of the HCV RNA dependent RNA polymerase identified two 168 member N-acyl pyrrolidine combinatorial mixture hits. Deconvolution and expansion of these mixtures by solid phase synthesis to establish initial
Autor:
Catherine E. Peishoff, John O. Link, Arun C. Kaura, Dashyant Dhanak, Kyle Elrod, Michael G. Darcy, George Burton, Dinubhai H. Shah, Richard M. Keenan, Lisa T. Christmann
Publikováno v:
Bioorganicmedicinal chemistry letters. 10(20)
A versatile synthetic route to a novel series of bis-imidazolemethanes designed to inhibit the hCMV protease has been developed and a series of potential metal binding inhibitors has been identified. In selectivity assays, the compounds were highly s
Publikováno v:
Journal of medicinal chemistry. 36(10)
The synthesis and phosphodiesterase (PDE) inhibitory profile of a series of imidazopyridines, including sulmazole and isomazole, on separated PDE isoenzymes are described. The results show that both sulmazole and isomazole are weak inhibitors of PDE