Eric E Boros

Summary

Affiliation: GlaxoSmithKline Research and Development
Country: USA

Publications

  1. ncbi request reprint Neuromuscular blocking activity and therapeutic potential of mixed-tetrahydroisoquinolinium halofumarates and halosuccinates in rhesus monkeys
    Eric E Boros
    GlaxoSmithKline Research and Development, Five Moore Drive, Research Triangle Park, North Carolina 27709, USA
    J Med Chem 46:2502-15. 2003
  2. doi request reprint Synthesis and antiviral activity of 7-benzyl-4-hydroxy-1,5-naphthyridin-2(1H)-one HIV integrase inhibitors
    Eric E Boros
    GlaxoSmithKline Research and Development, Five Moore Drive, Research Triangle Park, North Carolina 27709, USA
    J Med Chem 52:2754-61. 2009
  3. ncbi request reprint Hantzsch synthesis of pyrazolo[1',2':1,2]pyrazolo[3,4-b]pyridines: partial agonists of the calcitonin receptor
    Eric E Boros
    GlaxoSmithKline Research and Development, Five Moore Drive, Research Triangle Park, NC 27709, USA
    J Org Chem 70:5331-4. 2005
  4. doi request reprint Facile reductive amination of aldehydes with electron-deficient anilines by acyloxyborohydrides in TFA: application to a diazaindoline scale-up
    Eric E Boros
    GlaxoSmithKline Research and Development, Five Moore Drive, Research Triangle Park, North Carolina 27709, USA
    J Org Chem 74:3587-90. 2009
  5. ncbi request reprint Synthesis and HIV-integrase strand transfer inhibition activity of 7-hydroxy[1,3]thiazolo[5,4-b]pyridin-5(4H)-ones
    Eric E Boros
    GlaxoSmithKline Research and Development, Five Moore Drive, Research Triangle Park, NC 27709, USA
    Bioorg Med Chem Lett 16:5668-72. 2006
  6. doi request reprint Naphthyridinone (NTD) integrase inhibitors: N1 protio and methyl combination substituent effects with C3 amide groups
    Brian A Johns
    GlaxoSmithKline Research and Development, Infectious Diseases Therapy Area Unit, Five Moore Drive, Research Triangle Park, NC 27709, USA
    Bioorg Med Chem Lett 23:422-5. 2013
  7. pmc The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral
    Edward P Garvey
    Department of Virology, RC2 3983, GlaxoSmithKline, 5 Moore Dr, Research Triangle Park, NC 27709 3398, USA
    Antimicrob Agents Chemother 52:901-8. 2008
  8. doi request reprint Combining symmetry elements results in potent naphthyridinone (NTD) HIV-1 integrase inhibitors
    Brian A Johns
    GlaxoSmithKline Research and Development, Infectious Diseases Therapeutic Area Unit, Five Moore Drive, Research Triangle Park, NC 27709, USA
    Bioorg Med Chem Lett 21:6461-4. 2011
  9. doi request reprint Discovery of 6,7-dihydro-5H-pyrrolo[2,3-a]pyrimidines as orally available G protein-coupled receptor 119 agonists
    Subba R Katamreddy
    GlaxoSmithKline Research and Development, Five Moore Drive, Research Triangle Park, North Carolina 27709, USA
    J Med Chem 55:10972-94. 2012
  10. doi request reprint Discovery of a highly potent, nonabsorbable apical sodium-dependent bile acid transporter inhibitor (GSK2330672) for treatment of type 2 diabetes
    Yulin Wu
    GlaxoSmithKline Research and Development, Five Moore Drive, Research Triangle Park, North Carolina 27709, USA
    J Med Chem 56:5094-114. 2013

Collaborators

Detail Information

Publications13

  1. ncbi request reprint Neuromuscular blocking activity and therapeutic potential of mixed-tetrahydroisoquinolinium halofumarates and halosuccinates in rhesus monkeys
    Eric E Boros
    GlaxoSmithKline Research and Development, Five Moore Drive, Research Triangle Park, North Carolina 27709, USA
    J Med Chem 46:2502-15. 2003
    ..The NMB properties of 24a in rhesus monkeys led to its clinical evaluation as a possible alternative to succinylcholine...
  2. doi request reprint Synthesis and antiviral activity of 7-benzyl-4-hydroxy-1,5-naphthyridin-2(1H)-one HIV integrase inhibitors
    Eric E Boros
    GlaxoSmithKline Research and Development, Five Moore Drive, Research Triangle Park, North Carolina 27709, USA
    J Med Chem 52:2754-61. 2009
    ..Pharmacokinetic data in rats for one carboxamide analogue demonstrated oral bioavailability and reasonable in vivo clearance...
  3. ncbi request reprint Hantzsch synthesis of pyrazolo[1',2':1,2]pyrazolo[3,4-b]pyridines: partial agonists of the calcitonin receptor
    Eric E Boros
    GlaxoSmithKline Research and Development, Five Moore Drive, Research Triangle Park, NC 27709, USA
    J Org Chem 70:5331-4. 2005
    ..Oxidation of 10a-d to pyridines 11a-d and subsequent amide formation afforded the title compounds...
  4. doi request reprint Facile reductive amination of aldehydes with electron-deficient anilines by acyloxyborohydrides in TFA: application to a diazaindoline scale-up
    Eric E Boros
    GlaxoSmithKline Research and Development, Five Moore Drive, Research Triangle Park, North Carolina 27709, USA
    J Org Chem 74:3587-90. 2009
    ..Spectral data supported the tris(trifluoroacetoxy)borohydride anion (16) as the active reducing agent...
  5. ncbi request reprint Synthesis and HIV-integrase strand transfer inhibition activity of 7-hydroxy[1,3]thiazolo[5,4-b]pyridin-5(4H)-ones
    Eric E Boros
    GlaxoSmithKline Research and Development, Five Moore Drive, Research Triangle Park, NC 27709, USA
    Bioorg Med Chem Lett 16:5668-72. 2006
    ..Sub-micromolar enzyme inhibition of HIV integrase was achieved with several carboxamide analogs which were superior to their carboxylic ester congeners...
  6. doi request reprint Naphthyridinone (NTD) integrase inhibitors: N1 protio and methyl combination substituent effects with C3 amide groups
    Brian A Johns
    GlaxoSmithKline Research and Development, Infectious Diseases Therapy Area Unit, Five Moore Drive, Research Triangle Park, NC 27709, USA
    Bioorg Med Chem Lett 23:422-5. 2013
    ..The impact of substitution on ligand efficiency was considered and several compounds were advanced into in vivo pharmacokinetic studies ultimately leading to the clinical candidate GSK364735...
  7. pmc The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral
    Edward P Garvey
    Department of Virology, RC2 3983, GlaxoSmithKline, 5 Moore Dr, Research Triangle Park, NC 27709 3398, USA
    Antimicrob Agents Chemother 52:901-8. 2008
    ..Thus, based on all the data, GSK364735 exerted potent antiviral activity through the inhibition of viral DNA integration by interacting at the two-metal binding site within the catalytic center of HIV integrase...
  8. doi request reprint Combining symmetry elements results in potent naphthyridinone (NTD) HIV-1 integrase inhibitors
    Brian A Johns
    GlaxoSmithKline Research and Development, Infectious Diseases Therapeutic Area Unit, Five Moore Drive, Research Triangle Park, NC 27709, USA
    Bioorg Med Chem Lett 21:6461-4. 2011
    ..Effects of aryl and N1 substitutions are disclosed including the impact on protein binding adjusted antiviral activity...
  9. doi request reprint Discovery of 6,7-dihydro-5H-pyrrolo[2,3-a]pyrimidines as orally available G protein-coupled receptor 119 agonists
    Subba R Katamreddy
    GlaxoSmithKline Research and Development, Five Moore Drive, Research Triangle Park, North Carolina 27709, USA
    J Med Chem 55:10972-94. 2012
    ..Thus, 3 appeared to modulate the enteroinsular axis, improve glycemic control, and strengthen previous suggestions that GPR119 agonists may have utility in the treatment of type 2 diabetes...
  10. doi request reprint Discovery of a highly potent, nonabsorbable apical sodium-dependent bile acid transporter inhibitor (GSK2330672) for treatment of type 2 diabetes
    Yulin Wu
    GlaxoSmithKline Research and Development, Five Moore Drive, Research Triangle Park, North Carolina 27709, USA
    J Med Chem 56:5094-114. 2013
    ....
  11. ncbi request reprint Alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitors
    Alex G Waterson
    GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709 3398, USA
    Bioorg Med Chem Lett 16:2419-22. 2006
    ..In addition, the presence of a potential hydrogen bond donor appended to this ring was favored. Selected molecules in the series demonstrated some activity against human tumor cell lines...
  12. ncbi request reprint Exploration of the P2-P3 SAR of aldehyde cathepsin K inhibitors
    Eric E Boros
    Department of Medicinal Chemistry, GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709 3398, USA
    Bioorg Med Chem Lett 14:3425-9. 2004
    ..Exploration of the properties of the S2 and S3 subsites with a series of carbamate derivatized norleucine aldehydes substituted at the P2 and P3 positions afforded analogs with cathepsin K IC50s between 600 nM and 130 pM...
  13. ncbi request reprint Preclinical pharmacology of GW280430A (AV430A) in the rhesus monkey and in the cat: a comparison with mivacurium
    John J Savarese
    Department of Anesthesiology, Weill Medical College of Cornell University and New York Presbyterian Hospital, New York, New York 10021, USA
    Anesthesiology 100:835-45. 2004
    ..The neuromuscular, cardiovascular, and autonomic pharmacology of GW280430A is compared herein with that of mivacurium...