Zobrazeno 1 - 10
of 45
pro vyhledávání: '"Andrew Spaltenstein"'
Autor:
Jianjun Gan, Lou Yu, David A. Wilfret, Brad Shotwell, Jill Walker, Kimberly K. Adkison, Christian Voitenleitner, Daniel J. Lee, J. Kim, Sharon Baptiste-Brown, Mark Lovern, Amanda Mathis, Andrew Spaltenstein, Lee Moss
Publikováno v:
Clinical Pharmacology in Drug Development. 3:439-448
This first-time-in-human, randomized, double-blind, placebo-controlled, dose-escalation study assessed the safety, tolerability, pharmacokinetics, and antiviral activity of GSK2485852, a hepatitis C virus (HCV) NS5B inhibitor, in 27 chronically infec
Autor:
Andrew Maynard, Renae M. Crosby, Byron Ellis, Robert Hamatake, Zhi Hong, Brian A. Johns, Kirsten M. Kahler, Cecilia Koble, Anna Leivers, Martin R. Leivers, Amanda Mathis, Andrew J. Peat, Jeffrey J. Pouliot, Christopher D. Roberts, Vicente Samano, Rachel M. Schmidt, Gary K. Smith, Andrew Spaltenstein, Eugene L. Stewart, Pia Thommes, Elizabeth M. Turner, Christian Voitenleitner, Jill T. Walker, Greg Waitt, Jason Weatherhead, Kurt Weaver, Shawn Williams, Lois Wright, Zhiping Z. Xiong, David Haigh, J. Brad Shotwell
Publikováno v:
Journal of Medicinal Chemistry. 57:1902-1913
A boronic acid moiety was found to be a critical pharmacophore for enhanced in vitro potency against wild-type hepatitis C replicons and known clinical polymorphic and resistant HCV mutant replicons. The synthesis, optimization, and structure-activit
Autor:
Mark Edelstein, Jennifer Peckham, Wieslaw M. Kazmierski, Zhiping Xiong, Pat Wheelan, Robert Ferris, Andrew Spaltenstein, Maosheng Duan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:7401-7404
Modification of the acyl moiety in the CCR5 lead molecule 2 led to identification of several new classes of CCR5 antagonists. Antiviral activity and pharmacokinetic properties of the synthesized compounds were evaluated. Structure-activity relationsh
Autor:
Stephen Jenkinson, Pat Wheelan, Andrew Spaltenstein, Michael Thomson, Kristjan S. Gudmundsson, Richardson Leah D Aurora, John F. Miller
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:3026-3030
Using AMD070 as a starting point for structural modification, a novel series of isoquinoline CXCR4 antagonists was developed. A structure-activity scan of alternate lower heterocycles led to the 3-isoquinolinyl moiety as an attractive replacement for
Autor:
Michael Thomson, John F. Miller, Kristjan S. Gudmundsson, Elizabeth M. Turner, Stephen Jenkinson, Pat Wheelan, Andrew Spaltenstein
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:2125-2128
The lead optimization of a series of N-substituted benzimidazole CXCR4 antagonists is described. Side chain modifications and stereochemical optimization led to substantial improvements in potency and protein shift to afford compounds with low nanomo
Autor:
Pamela L. Golden, Ronald George Sherrill, John F. Miller, Andrew Spaltenstein, Phiroze Sethna, Elizabeth M. Turner, Karen Rene Romines, Kevin W. Brown, Robert J. Harvey, Kristjan S. Gudmundsson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:256-259
The identification and optimization of a series of substituted tetrahydro-β-carbolines with potent activity against human papillomavirus is described. Structure–activity studies focused on the substitution pattern and chirality of the β-carboline
Autor:
John G. Catalano, Andrew Spaltenstein, Kristjan S. Gudmundsson, Michael Thomson, Pat Wheelan, Stephen Jenkinson, Boggs Sharon Davis, Angilique Svolto
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:6399-6403
Synthesis of several novel imidazopyridine-5,6,7,8-tetrahydro-8-quinolinamine derivatives with potent activity against HIV are described. Synthetic approaches allowing for variation of the substitution pattern are outlined and resulting changes in an
Autor:
Istvan Kaldor, Ronald George Sherrill, Furfine Eric Steven, David J. Reynolds, John F. Miller, Richard J. Hazen, Michael Stephen Brieger, Andrew Spaltenstein
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:3496-3500
A novel series of tyrosine-derived HIV protease inhibitors was synthesized and evaluated for in vitro antiviral activity against wild-type virus and two protease inhibitor-resistant viruses. All of the compounds had wild-type antiviral activities tha
Autor:
Lois L. Wright, William J. Bock, Richard J. Hazen, Francesco G. Salituro, Furfine Eric Steven, Merrick R. Almond, Andrew Spaltenstein, Roger D. Tung, Wieslaw M. Kazmierski, Darryl Cleary
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:1159-1162
A novel series of HIV protease inhibitors containing cyclic P1/P2 scaffolds has been synthesized and evaluated for biological activity. The trans 3,5-dibenzyl-2-oxo pyrrolidinone ring system resulted in a 50 pM enzyme inhibitor against HIV protease i
Autor:
John W. Seal, Dan Todd, Banka Anna L, Luz H. Carballo, Zhiping Xiong, Lisa L. Stroup, Amanda Mathis, Zhi Hong, Jeffery J. Pouliot, Pek Yoke Chong, Michael Youngman, Robert Hamatake, Daniel J. Price, Jing Fang, Katrina L. Creech, Andrew Spaltenstein, John G. Catalano, Christopher Don Roberts, J. Brad Shotwell, Andrew J. Peat, Vincent W.-F. Tai, John F. Miller, Sylvia Furst, Huichang Zhang
Publikováno v:
Journal of medicinal chemistry. 57(5)
We describe the preclinical development and in vivo efficacy of a novel chemical series that inhibits hepatitis C virus replication via direct interaction with the viral nonstructural protein 4B (NS4B). Significant potency improvements were realized