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A number of publications have reported the coupling of carboxylic acids to Merrifield resin via the cesium salt method and the esterification of Wang resin using carbodiimide either via the isourea method or the symmetrical anhydride method. Reaction times using conventional conditions have been reported to be rather long so we have investigated the effects of microwave irradiation towards both of these reactions using benzoic acid derivatives.

In stem cell cultures there is the possibility of infectious disease transmission to the recipients. Any microbial contamination of the donor`s biological products or introduced during the manufacturing process can potentially present a serious hazard to the recipients. The majority of potential contaminants are mycoplasma and other bacterias, yeasts and fungi. Moreover, viral and prion contamination of cell cultures and “feeder” cells is also a common risk.

Experimental approaches using short interfering RNA (siRNA) molecules to specifically silence gene expression have become more widely used in recent years. As for all techniques in molecular and cellular biology, the importance of protocol optimization and the use of appropriate controls cannot be overestimated.

The absorption of orally administered compounds is largely determined by their ability to cross the gastrointestinal tract. Cell culture models can be intensive and limited to a narrow pH range. Assays using artificial membranes, such as PAMPA (parallel artificial membrane permeation assay) can be used as an alternative approach to assess in vitro transcellular passive permeation.

For pharmaceutical companies it is not only essential to identify HERG interacting compounds early during the drug discovery and development process, but also to understand potential effects of compounds on the cardiac action potential. This helps to increase the safety for patients, and to avoid the costs of unsuccessful projects in later phases.

The prevalence and clinical implications, of mechanism-based CYP450 inhibition has placed greater emphasis on the early detection of compounds with this potential. We have developed and validated a high throughput reversible CYP450 inhibition assay using human liver microsomes and industry recommended probe substrates.

With the increasing application of high-throughput assays for the determination of the in vitro ADME properties of compounds in lead identification and optimization, there is a growing need for efficient and cost-effective methods for interpreting theresulting data to enable well-informed selection to be made for compound progression.

In recent work we have reported the generation of a diverse library of DHPMs, employing an automated, sequential microwave-assisted solution phase strategy. We now present the high-speed microwave scaffold decoration around the DHPM heterocyclic core exploiting the diversity on at least six positions.

Microwave-assisted organic synthesis in near-critical water (NCW) in the 270-300 °C temperature range has been investigated in a dedicated multimode microwave reactor utilizing heavy-walled quartz reaction vessels. Several different known transformations such as the hydrolysis of esters or amides, the hydration of alkynes, Diels-Alder cycloadditions, pinacol rearrangements, and the Fischer indole synthesis were successfully performed in microwave-generated NCW without the addition of an acid

The readily available and broadly functionalized 2-azadiene system of the 2(1H)-pyrazinones easily undergo inter- and intramolecular Diels-Alder reactions with a wide range of dienophiles providing convenient routes to specifically substituted heterocycles. The reactions in this series are known to be rather sluggish, requiring long reaction times, high temperatures and even sometimes high pressures. Since speed is generally recognized as an important factor in high-throughput synthesis, we have