High-throughput methods

Recent studies of Pt supported on titania synthesized using the high throughput method on arrays have also revealed a particle size dependence of the ORR... 

High throughput methods have increased our capacity for appropriate candidate compounds selection and also for developing libraries of novel compounds from which such candidates can be selected. Chapter 7 discusses the use of solid-phase synthesis for the high throughput production of peptides and other small molecules. In addition, as discussed in Chapter 6 on peptidomimetics, the swift production of novel leads holds considerable promise for future discovery of novel therapeutic agents. 

A high-throughput method using a 96-well microtiter plate format and plate UV spectrophotometry has been described [26]. Solubilities at a single pH, or at <12 pH values can be determined, using one of two methods. 

At higher reaction temperatures (>300°C), micro- or meso-porous materials and/or oxides containing transition metals are preferable. The performances are considerably dependent on the type of reductant, besides the characteristics of the catalyst and the type of transition metal. Although all possible combinations have been explored, including the usage of high-throughput methods, identification of a suitable catalyst formulation active in HC-SCR under practical conditions, especially to decrease by more than... 

Volume 431. Translation Initiation Cell Biology, High-Throughput Methods, and Chemical-Based Approaches Edited by Jon Lorsch... 

A high-throughput method for the monoacylation of 7-amino-5-aryl-6-cyanopyr-ido[2,3-d]pyrimidines with acid chlorides has been reported by Nicewonger and his team at ArQule (Scheme 6.157) [303], Since incomplete conversions were achieved... 

High Throughput Method for the Discovery of Chain Shuttling Catalyst Systems. 74... 

Utility of Multisorbent Extraction for SPE High-Throughput Method Development... 

MS has recently been used to measure compounds with significant levels of impurities and solubilities below the quantitation limits of other methods. Guo et al.46 described the use of LC/MS for solubility measurements in buffer solutions in a 96-well plate. Fligge et al.47 discussed an automated high-throughput method for classification of compound solubility. They integrated a Tecan robotic system for sample preparation in 384-well plates and fast LC/MS for concentration measurement. This approach is limited by LC/MS throughput. 

A linear calibration curve for carvedilol in plasma was constructed over a range of 1 to 80 ng/mL. The correlation coefficient exceeded 0.999. Intra-day and inter-day coefficients of variation were 1.93 and 1.88%, respectively. The average carvedilol recovery was 98.1%. The limit of quantification was 1 ng/mL. This high-throughput method enabled the analysis of more than 600 plasma samples without significant loss of column efficiency. 

Epirubicin — Anthracyclines have been used in cancer chemotherapy for more than 30 years and epirubicin (EPI) is one of the most widely used agents.55 Li et al. developed a high-throughput method for the analysis of epirubicin in human plasma using UPLC-MS/MS.56 A Waters Acquity UPLC system was coupled with a Micromass Quattro Premier MS. The stationary phase was a Waters Acquity BEH C18 column (50 x 2.1 mm, 1.7 jum). The column was maintained at 30°C. Solvent A was 0.1% formic acid in water and solvent B was acetonitrile. The mobile phase was delivered at a flow of 0.20 mL/min in a step gradient mode at 85% solvent A at 0 min, 70% solvent A at 1.00 min, and 85% solvent A from 2.50 to 4.00 min. Epidaunorubicin (EPR) was the IS. 

High-throughput methods for catalyst screening and optimization, as described in the literature even for hydrogenations [35], are not suitable for kinetic analyses in most cases. 

In an attempt to find new active ORR catalysts, Liu et al. used a high-throughput method to screen both noble and non-noble metal binary catalysts for ORR in both acidic and methanol-containing media.223 Of the non-noble metal catalysts (CrCo, CrCu, CrFe, CrNi) none were found to be active in H2S04 or H2S04/methanol. 

Estimation or measurement of pKa is important to understand the state of ionization of the drug under physiological conditions and to evaluate salt-forming ability.27 Log P determines the partitioning of a drug between an aqueous phase and a lipid phase (i.e., lipid bilayer). Log P and acid pKa can be theoretically estimated with reasonable accuracy.14,28,29 High-throughput methods are also available for measurement of log P30 and pKa.31... 

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