Zobrazeno 1 - 10
of 52
pro vyhledávání: '"John R. Harding"'
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 59:250-254
[(14) C]-AZD1152 (barasertib) drug substance was prepared in order to support a hADME study that was to be dosed as an intravenous infusion to patients with acute myeloid leukaemia. A long patient recruitment time (1-2 years) was expected, and becaus
Autor:
Rebecca Urbanek, J. Richard Heys, Peter N. Dorff, Timothy Blake, Scott W. Landvatter, James E. Hall, Charles S. Elmore, Mark E. Powell, Glen Ernst, John R. Harding, David A. Killick
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 57:342-349
In support of a program to develop an alpha 7 agonist as a treatment for Alzheimer's disease, three drug candidates, 1, 2, and 3, were prepared in labeled forms. Compound 1 was prepared in C-14 labeled form by lithiation of [2,6-(14)C2]2-chloropyridi
Autor:
Mazhar Iqbal, Caroline H. Johnson, Jeremy K. Nicholson, Lisa Iddon, Xiaoli Meng, Sunil Sarda, John C. Lindon, Elin S. Karlsson, Ian D. Wilson, Andrew V. Stachulski, John R. Harding
Publikováno v:
Rapid Communications in Mass Spectrometry. 24:3043-3051
The use of high-performance liquid chromatography/mass spectrometry (HPLC/MS) and proton nuclear magnetic resonance (1H NMR) spectroscopy for the kinetic analysis of acyl glucuronide (AG) isomerisation and hydrolysis of the 1-β-O-acyl glucuronides (
Publikováno v:
Tetrahedron. 66:537-541
N-Glucuronides, of various structural types, are frequently encountered as drug metabolites. Efficient chemical synthesis of these compounds, both as analytical standards and for toxicological investigation, is therefore an important goal. Earlier sy
Autor:
Andrew V. Stachulski, John Bacsa, John R. Harding, Lisa Iddon, Ryan A. Bragg, Anthony J. Kirby, Chandrakala Pidathala
Publikováno v:
Tetrahedron. 65:6396-6402
We report convenient syntheses of anomeric quaternary ammonium β-glucosides in both protected and deprotected forms, together with X-ray structural investigations of two of the products. Both the quaternisation of a protected anomeric N,N-(dimethyla
Autor:
Rachel J. Walsh, Scott W. Martin, Dominic P. Williams, Raimund M. Peter, Emma E. Graham, Charlotte Hirst, B. Kevin Park, Martin Wild, Ian D. Wilson, John R. Harding, James L. Maggs, J. Gerry Kenna
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 326:657-671
Methapyrilene (MP), a 2-thiophene H(1)-receptor antagonist, is a model toxicant in the genomic and proteomic analyses of hepatotoxicity. In rats, it causes an unusual periportal necrosis that is hypothetically attributed to chemically reactive and cy
Autor:
Jennifer A. Perrie, B. Kevin Park, Andrew V. Stachulski, James L. Maggs, Elizabeth R. Bowkett, John R. Harding
Publikováno v:
Tetrahedron. 63:7596-7605
Acyl glucuronides are key metabolites for many carboxylic acid-containing drugs, notably those of the non-steroidal anti-inflammatory class. In the processes of drug safety assessment and new drug development, it is essential that acyl glucuronides,
Autor:
Russell J. Cox, Thomas J. Simpson, John R. Harding, Nick Bushby, David O. Rees, Christine L. Willis
Publikováno v:
ChemBioChem. 8:46-50
Autor:
Thomas J. Simpson, John R. Harding, Lorraine C. Axford, Angela Jordan, Yvonne O'Connell, Christine L. Willis
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 50:338-341
Syntheses of isotopically labelled putative biosynthetic intermediates to the natural products monocerin 1, hectochlorin 2 and strobilurin A 3 are described. For the preparation of [9,10- 13 C 2 ]dihydroisocoumarin 10, a stereoselective aldol condens
Autor:
John R. Harding
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 50:927-932
Synthetic isotope chemistry has played a key role in the discovery and development of candidate drugs for over 40 years at Alderley Park, UK. This review highlights the range of isotopically labelled compounds that have been synthesized and the appli