Zobrazeno 1 - 10
of 74
pro vyhledávání: '"Igor Goljer"'
Autor:
Bianca Squillaci, Dung Nguyen, Mohammad Hossain, Clara Andonian, Mally Lev, Kitaw Negash, May Ho, Courtney Tiffany, Jill L. Pirhalla, Cathy L. Chen, Igor Goljer, Clive Felgate, Ernest Schubert
Publikováno v:
Xenobiotica. 46:683-702
1. GSK2140944 is a novel bacterial topoisomerase inhibitor in development for the treatment of bacterial infections. The metabolism and disposition in healthy human subjects was investigated. 2. Six male subjects received [(14)C] GSK2140944 orally (2
Autor:
L. A. Jones, Jianjun Gan, Joseph Horton, C. L. Moseley, David A. Wilfret, Yu Lou, Jill Walker, M. de Serres, Kimberly K. Adkison, Stephen Castellino, Igor Goljer, Amanda G. Culp, William Spreen
Publikováno v:
Antimicrobial Agents and Chemotherapy. 57:5037-5044
GSK2336805 is an orally bioavailable hepatitis C virus (HCV) inhibitor working through an NS5A-mediated mechanism. This first-time-in-human study was conducted to assess the safety, tolerability, pharmacokinetics, metabolism, and efficacy of GSK23368
Autor:
Paul Savina, Shuguang Chen, Ivy Song, Amanda G. Culp, Lee Moss, Stephen Castellino, David S. Wagner, Stephen C. Piscitelli, Igor Goljer, Yu Lou, Sherene S. Min, Julie Borland
Publikováno v:
Antimicrobial Agents and Chemotherapy. 57:3536-3546
The pharmacokinetics, metabolism, and excretion of dolutegravir, an unboosted, once-daily human immunodeficiency virus type 1 integrase inhibitor, were studied in healthy male subjects following single oral administration of [ 14 C]dolutegravir at a
Autor:
Baihua Hu, Elaine Quinet, Irene Feingold, Igor Goljer, Thomas J. Berrodin, Mark J. Evans, James W Jetter, Jay Wrobel, Rayomand J. Unwalla, Michael D Basso, Annika Goos Nilsson, Anna Wilhelmsson
Publikováno v:
Journal of Medicinal Chemistry. 53:3296-3304
A series of phenyl sulfone substituted quinoxaline were prepared and the lead compound 13 (WYE-672) was shown to be a tissue selective LXR Agonist. Compound 13 demonstrated partial agonism for LXRbeta in kidney HEK-293 cells but did not activate Gal4
Autor:
Darlene C. Deecher, Puwen Zhang, An T. Vu, Jenifer A. Bray, Rebecca Dooley, Stephen Todd Cohn, Igor Goljer, Paige Erin Mahaney, Grace H. Johnston, Jennifer Leiter, Terefenko Eugene Anthony, Eugene John Trybulski, William Jay Moore
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:2464-2467
A series of 3-(arylamino)-3-phenylpropan-2-olamines was prepared and screened for their ability to inhibit monoamine reuptake. A number of analogues displayed significant dual norepinephrine and serotonin reuptake inhibition. Compounds in this class
Autor:
Igor Goljer, Jeffrey C. Pelletier, Diane S. Andraka, Linda Shanno, Daniel M. Green, Murty Chengalvala, Warren W. Hurlburt
Publikováno v:
Journal of Combinatorial Chemistry. 11:117-125
2-Trifluoromethyl-4-aminobenzimidazoles were previously identified by screening to be active antagonists of the gonadotropin releasing hormone receptor (GnRH-R). Structure activity relationships and diversity oriented synthesis are shown here in grea
Autor:
Li Di, Leonard A. McDonald, Mairead Young, Lisa Nogle, Dahui Zhou, Brian L. Marquez, Mei-Yi Zhang, William L. Watts, Frank E. Koehn, Alvin C. Bach, Yanxuan Cai, Alan G. Sutherland, Neal Byrne, Guy T. Carter, Michael Z. Kagan, Edward H. Kerns, Mark Tischler, Carl J. Balibar, Oliver J. McConnell, Igor Goljer, Gerhard Schlingmann, Yanan He, Don Herold, Douglas M. Ho, Michael Chlenov, Christopher J. Petucci, R. Thomas Williamson, Gregory J. Tawa, Yingru Zhang, Vasilios Marathias, Christina M. Kraml, Kristi Fan
Publikováno v:
Chirality. 19:658-682
The application of Chiral Technology, or the (extensive) use of techniques or tools for the determination of absolute stereochemistry and the enantiomeric or chiral separation of racemic small molecule potential lead compounds, has been critical to s
Autor:
Paige E. Mahaney, Matthew L. Crawley, Igor Goljer, Douglas John Jenkins, Lisa Nogle, Rebecca Dooley, John F. Mehlmann
Publikováno v:
Organic Letters. 8:5837-5840
The first efficient and regioselective palladium-catalyzed cyclization of internal alkynes and 2-amino-3-iodoacrylates to give moderate to excellent yields of highly functionalized pyrroles has been developed. This approach is applicable to a range o
Publikováno v:
Magnetic Resonance in Chemistry. 43:512-519
A high-resolution, phase-sensitive, natural abundance F2-coupled 1H-13C HSQC (F2HSQC) NMR experiment was developed to measure simultaneously both (n)D(HH) and 1D(CH) residual dipolar couplings (RDCs) of small molecules present in a chiral polypeptide
Publikováno v:
Magnetic Resonance in Chemistry. 34:S47-S54
The structures of duplex DNAs containing damaged sites can be determined by the combined use of NMR and restrained molecular dynamics. The NMR of DNAs containing abasic sites can be challenging since there are two equilibrating forms of the abasic si