Zobrazeno 1 - 10
of 29
pro vyhledávání: '"Scott L. Harbeson"'
Autor:
Scott L. Harbeson, Christopher L. Brummel, Dario Doller, Julie F. Liu, Robert H. Silverman, Roger D. Tung
The use of deuterium substitution in an effort to produce kinetic isotope effects (KIEs) that favorably alter pharmacokinetics and metabolism in drug discovery has accelerated in the last decade. While the effects of deuteration remain highly experim
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ea2fbe425fc282af194b33f639572cfb
https://doi.org/10.1016/bs.armc.2017.08.010
https://doi.org/10.1016/bs.armc.2017.08.010
Autor:
Lijun Wu, Sunanda Vedananda, Roger D. Tung, Virginia Braman, Scott L. Harbeson, Changfu Cheng
Publikováno v:
Journal of Mass Spectrometry. 48:1019-1031
Atazanavir (Reyataz(®)) is an important member of the HIV protease inhibitor class. Because of the complexity of its chemical structure, metabolite identification and structural elucidation face serious challenges. So far, only seven non-conjugated
Autor:
Lijun Wu, Roger D. Tung, Changfu Cheng, Scott L. Harbeson, Robert E. Zelle, Gary W. Bridson, Richard Gallegos
Publikováno v:
Journal of Mass Spectrometry. 48:640-650
Atazanavir (marketed as Reyataz®) is an important member of the human immunodeficiency virus protease inhibitor class. LC-UV-MSn experiments were designed to identify metabolites of atazanavir after incubations in human hepatocytes. Five major (M1
Publikováno v:
Drug Repositioning: Bringing New Life to Shelved Assets and Existing Drugs
Autor:
Craig E. Masse, Adam J. Morgan, Gary W. Bridson, Vinita Uttamsingh, Roger D. Tung, Sophia Nguyen, Scott L. Harbeson
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 54:613-624
As part of an ongoing effort to apply the Deuterated Chemical Entity Platform (DCE Platform™) to clinically validated drugs,the synthesis of deuterated analogs of the hepatitis C virus protease inhibitor boceprevir was carried out. The devisedsynth
Autor:
J. A. Malikayil, Scott L. Harbeson
Publikováno v:
International Journal of Peptide and Protein Research. 39:497-505
The hexapeptide [cyclo(Leu1 psi(CH2NH2)Leu2-Gln3-Trp4-Phe5-Gly6)]+1 is a potent antagonist of neurokinin A activity in tissues of hamster urinary bladder. The solution conformation of this cyclic hexapeptide has been characterized by the combined use
Autor:
Gary W. Bridson, Roger D. Tung, Richard Gallegos, Vinita Uttamsingh, David S. Wells, Changfu Cheng, Robert E. Zelle, Julie F. Liu, Philip B. Graham, Scott L. Harbeson
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 354(1)
Selective deuterium substitution as a means of ameliorating clinically relevant pharmacokinetic drug interactions is demonstrated in this study. Carbon-deuterium bonds are more stable than corresponding carbon-hydrogen bonds. Using a precision deuter
Autor:
Robert B. Perni, Yu-Ping Luong, Scott L. Harbeson, Pravin Chaturvedi, Gurudatt Chandorkar, John A. Thomson, Susan J. Almquist, Yunyi Wei, Randal Byrn, B. Govinda Rao, Gururaj Kalkeri, Kirk Dinehart, Ann D. Kwong, William P. Taylor, Cynthia A. Gates, Roger D. Tung, Kai Lin, Chao Lin, Lawrence F. Courtney, Angela D. Heiser, Caroline Decker, Elaine Kolaczkowski
Publikováno v:
Antimicrobial Agents and Chemotherapy. 50:899-909
VX-950 is a potent, selective, peptidomimetic inhibitor of the hepatitis C virus (HCV) NS3-4A serine protease, and it demonstrated excellent antiviral activity both in genotype 1b HCV replicon cells (50% inhibitory concentration [IC 50 ] = 354 nM) an
Autor:
Cynthia A. Gates, John A. Thomson, Kevin M. Cottrell, Yu P. Luong, Scott L. Harbeson, Robert B. Perni, John H. Van Drie, David D. Deininger, Roger D. Tung, Shawn D. Britt, Chao Lin, Janos Pitlik, Luc J. Farmer, John J. Court, Yunyi Wei, John Maxwell, Kai Lin, Bhisetti Govinda Rao, Lawrence F. Courtney, Wayne C. Schairer
Publikováno v:
Letters in Drug Design & Discovery. 2:497-502
Autor:
Kai Lin, Joseph L. Kim, Yu-Ping Luong, Janos Pitlik, Wayne C. Schairer, Chao Lin, Roger D. Tung, Robert B. Perni, John A. Thomson, John Maxwell, Luc J. Farmer, Kevin M. Cottrell, Murcko Mark A, Lawrence F. Courtney, Cynthia A. Gates, John J. Court, John H. Van Drie, David D. Deininger, Wilson Keith P, B. Govinda Rao, Scott L. Harbeson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:1939-1942
We recently described the identification of an optimized α-ketoamide warhead for our series of HCV NS3·4A inhibitors. We report herein a series of HCV protease inhibitors incorporating 3-alkyl-substituted prolines in P2. These compounds show except