|The use of Benzyl Esters in the Synthesis of 1ß-O-Acyl Glucuronides by Selective Acylation|
Elizabeth R. Bowkett, B. Kevin Park and Andrew V. Stachulski
Acyl glucuronides are key phase 2 metabolites for many carboxylic acid-containing drugs, notably of non-steroidal anti-inflammatory agents (NSAIDs).1 It is important to synthesise acyl glucuronides in pure form, and especially as single 1ß-anomers, for bioevaluation during drug discovery and development. Acyl glucuronides are reactive species: they may react by hydrolysis or displacement with other nucleophiles or by acyl migration followed by condensation with amines.
|Multicolor Detection of CD45 on Human Monocytes with Quantum Dots in a High-Throughput Format|
Paul Wylie, John Budd and Marcel Bruchez
Multicolor quantum dot probes emitting from 525 to 705 nm can be effectively excited with a single 488 nm laser, resulting in signals equal to the best organic dyes, but that are cleanly discriminated with simple color filters. Using a plate based 4-color laser scanning system with a single 488 or 405 nm laser for excitation, we have detected the binding of quantum dot conjugates to CD45 on human monocytes.
|Optimizing the hERG Assay on the PatchXpress 7000A System for Compounds that Demonstrate Non-specific Binding|
Iris Yang, Naibo Yang, Cathy Smith-Maxwell, Claire Quinn, Kirsty Macfarlane and David Yamane
Eight compounds, astemizole, pimozide, dofetilide, cisapride, terfenadine, flunarizine, quinidine and imipramine were used to evaluate the effect of different assay conditions to overcome the effects of non-specific binding in our hERG assay on the PatchXpress 7000A system.
|Reducing the Synthetic Burdens of Lead Structure Optimization: A Novel Software-Aided Approach|
Karim Kassam, Ryan Sasaki and Michel R.J. Hachey
At the later stages of drug optimization it is beneficial to augment the select ADME properties of leads by making small structural changes that do not introduce any negative effects on the activity or toxicity profiles. By combining physicochemical property predictors and a critically evaluated database of biologically-acceptable substituents, the synthetic chemist can evaluate and reduce the number of derivative compounds that need to be synthesized to achieve optimal drug-like properties.
|Development of an Analytical Data Management System (ADMS) to Accelerate the Selection of a Suitable API Form Through Salt and Polymorph Screening|
Raeann Wu, Peter Karpinski, Patrick Drumm, Karim Kassam, Michel R.J. Hachey and Michael Boruta
In this work, we discuss the acceleration of the preformulation process through the use of modern software systems. The data system discussed can read, process, store, retrieve, visualize and report a wide variety of data type—XRD, Raman, HPLC, NMR, TGA, DSC, chemical structures, properties and images—in a centralized and homogeneous way. A pilot study at a pharmaceutical company demonstrated possible time savings between 20% and 80% at various points in the preformulation workflow.
|High Throughput Automated High Content Screening using a BioCube™ System and Microplate Cytometry|
Wayne Bowen, Jason Quarles and Michael Catalano
Here, we model the integration of the Protedyne BioCube System and the Acumen Explorer for practical high-throughput, high content screening of protein kinases.
|Diagnostic Genotyping of Drug Metabolising Enzyme Genes on Microarray: The DrugMEt™ Pharmacogenetic IVD Test |
Hendolin PH, PhD, U Ristonmaa, MSc, A Liikola, MSc, P Kolu, MSc, T Varis, LabTech, A Lehtelä, LabTech. and V-P Korhonen, PhD
A microarray test for in vitro diagnostic use that contains 27 SNPs from 8 different genes with a proven role in the metabolism of major drugs and that may be processed using regular laboratory instrumentation and a range of different scanners.
|Carbon Nanotubes by Microwave Plasma Enhanced Chemical Vapor Deposition|
M. Maschmann, A. Goyal, Z. Iqbal, T.S. Fisher, R. Gat
MICROWAVE Plasma generates radical density characteristic of 2000C at much lower effective temperature and can be highly ionized (Low pressure ECR mode) or highly neutral (high pressure mode).
|Metabonomics for MolPAGE Discovering Diabetes Biomarkers|
K. Magnus Åberg, Mark Jairaj, Henrik Toft Pedersen, Dorrit Baunsgaard
MolPAGE (Molecular Phenotyping to Accelerate Genomic Epidemiology) is an EU consortium with almost twenty collaborating universities and companies throughout Europe. One of the aims of MolPAGE is to find early onset biomarkersfor type 2 diabetes (T2DM) and cardio-vascular diseases(CVD).
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