COMMENTS |
ChemRx div., Yan Bing, director of analytical sciences “Parameters like identity, purity & concn are crucial to define the quality of a combinatorial library, & the quality of a library is absolutely essential for the success of biological screening”. The present system “has streamlined the processes of obtaining all these important parameters into a single measurement. This technology & any modified & derivative versions will make a great impact on the advance of combinatorial synthesis” |
TECHNOLOGY |
A new system has been developed for evaluating in a single experiment, the IDENTITY, PURITY & CONCENTRATION of combinatorial LIBRARY compds made by PARALELL synthesis. In the system, HPLC separates components of synthetic samples that are arrayed on microtiter plates. The eluent is first analyzed by UV-visible Photo Diode Array (PDA) detector & is then directed to 3 other analyzers – a Evaporative Light-Scattering Detector (ELSD), a ChemiLuminescent Nitro gen Detector (CLND) & a Time-Of-Flight Mass Spectrometry (TOFMS) unit. It was devised to solve a common parallel synthesis problem: Target compds are produced in a range of yields & purities, making it difficult to screen them for biol activity Scientists generally address this problem by purifying samples before screening or by characterizing “hits” after screening. But both approaches can be time-consuming & inefficient. The present technique identifies library compds & determines their purity & concn in one procedure, potentially speeding combinatorial studies. One of its advantages is that TOFMS has high mass accuracy, making it possible to rigorously confirm library compd’s exact molecular formula & to identify synthetic impurities & side prodts mixed in with it. And CLND can determine the concn of any N-contg compd., without any need for comparison with primary standards, if the compd.’s molecular formula is known from the TOFMS step. |
UPDATE | 03.02 |
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