Research Topics
| Eric E BorosSummaryAffiliation: GlaxoSmithKline Research and Development Country: USA Publications
| Collaborators
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Detail Information
Publications
Neuromuscular blocking activity and therapeutic potential of mixed-tetrahydroisoquinolinium halofumarates and halosuccinates in rhesus monkeysEric 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...
Synthesis and antiviral activity of 7-benzyl-4-hydroxy-1,5-naphthyridin-2(1H)-one HIV integrase inhibitorsEric 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...- Facile reductive amination of aldehydes with electron-deficient anilines by acyloxyborohydrides in TFA: application to a diazaindoline scale-upEric 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... - Hantzsch synthesis of pyrazolo[1',2':1,2]pyrazolo[3,4-b]pyridines: partial agonists of the calcitonin receptorEric 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... - Synthesis and HIV-integrase strand transfer inhibition activity of 7-hydroxy[1,3]thiazolo[5,4-b]pyridin-5(4H)-onesEric 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... - Naphthyridinone (NTD) integrase inhibitors: N1 Protio and methyl combination substituent effects with C3 amide groupsBrian A Johns
GlaxoSmithKline Research and Development, Infectious Diseases Therapy Area Unit, Five Moore Drive, Research Triangle Park, NC 27709, USA Electronic address
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... 
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviralEdward 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...- Combining symmetry elements results in potent naphthyridinone (NTD) HIV-1 integrase inhibitorsBrian 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... - Discovery of 6,7-Dihydro-5H-pyrrolo[2,3-a]pyrimidines as Orally Available G Protein-Coupled Receptor 119 AgonistsSubba R Katamreddy
GlaxoSmithKline Research and Development, Five Moore Drive, Research Triangle Park, North Carolina 27709, United States
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... - Alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitorsAlex 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... - Exploration of the P2-P3 SAR of aldehyde cathepsin K inhibitorsEric 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... - Preclinical pharmacology of GW280430A (AV430A) in the rhesus monkey and in the cat: a comparison with mivacuriumJohn 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...