High Throughput Analysis for Early Drug DiscoveryJames Kyranos Elsevier, 2004 M09 18 - 204 pages High Throughput Analysis for Early Drug Discovery offers concise and unbiased presentations by synthetic and analytical chemists who have been involved in creating and moving the field of combinatorial chemistry into the academic and industrial mainstream. Since the synthetic method often dictates the appropriate types of analysis, each chapter or section begins with a description of the synthesis approach and its advantages. The description of various combinatorial and high-throughput parallel synthesis techniques provide a relevant point of entry for synthetic chemists who need to set up appropriate characterisation methods for his/her organisation. This is an invaluable resource for all organic and analytical chemists in the pharmaceutical, agrochemical, and biotechnology fields who are either involved in, or beginning to investigate combinatorial techniques to increase overall efficiency and productivity.
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Page 4
... observed MW MW Figure 1.2 Single bead library QA process. One approach to characterizing the large encoded libraries is through library QA analysis. By combining LC/MS analysis with tag decode analysis, the physical existence of the ...
... observed MW MW Figure 1.2 Single bead library QA process. One approach to characterizing the large encoded libraries is through library QA analysis. By combining LC/MS analysis with tag decode analysis, the physical existence of the ...
Page 5
... observed compounds and synthons in a library. 4 SYNTHESIS OF THE ENCODED STATINE AMIDE LIBRARY The encoded solid-phase synthesis of the statine amide library 1 (Scheme 1.1 and Fig. 1.3), has been previously described.” Statine library 1 ...
... observed compounds and synthons in a library. 4 SYNTHESIS OF THE ENCODED STATINE AMIDE LIBRARY The encoded solid-phase synthesis of the statine amide library 1 (Scheme 1.1 and Fig. 1.3), has been previously described.” Statine library 1 ...
Page 12
... observed for the replicate structures, together with the consistent composite p values of the three QA analyses, provide a satisfactory level of validation for this statistical-based approach to library quality assessment. Examination ...
... observed for the replicate structures, together with the consistent composite p values of the three QA analyses, provide a satisfactory level of validation for this statistical-based approach to library quality assessment. Examination ...
Page 15
... observed. There was sufficient quantity of material at this stage to obtain UV data for many of the intermediates, which showed > 85% purity (unpublished observation). Specifically, synthon B46 gave a p > 80% indicating chemical failure ...
... observed. There was sufficient quantity of material at this stage to obtain UV data for many of the intermediates, which showed > 85% purity (unpublished observation). Specifically, synthon B46 gave a p > 80% indicating chemical failure ...
Page 18
... observed in sub-library 8j, defined by the synthon pair C2/D10, followed by sub-library 8a, defined by the synthon pair C1/D1. Subsequently, two additional follow-up copies of sub-library 8j were screened one compound per well (5040 ...
... observed in sub-library 8j, defined by the synthon pair C2/D10, followed by sub-library 8a, defined by the synthon pair C1/D1. Subsequently, two additional follow-up copies of sub-library 8j were screened one compound per well (5040 ...
Contents
Chapter 2 Analysis of a Combinatorial Library Synthesized Using a SplitandPool Irori MicroKan Method for Development and Production | 37 |
Chapter 3 High Throughput Flow Injection AnalysisMass Spectrometry | 57 |
Chapter 4 High Throughput Flow Injection AnalysisMass Spectrometry for Combinatorial Chemistry Using Electrospray Ionization Atmospheric Pres... | 73 |
Chapter 5 Purity and Quantity Determination of Parallel Synthesis Compound Libraries | 95 |
Chapter 6 High Throughput Parallel LCMSELSD of Combinatorial Libraries Using the EightChannel LCT System with MUX Technology | 113 |
Chapter 7 Purification and Analysis of Parallel Libraries | 125 |
Chapter 8 Screening SingleBead Combinatorial Libraries using Capillary HPLC and MALDITOFMS | 147 |
Chapter 9 The Role of NMR in the Analysis of Chemical Libraries | 163 |
Subject Index | 183 |
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Common terms and phrases
acid activity addition allow amount Anal analysis analytical APCI application approach approximately automated autosampler beads channel characterization Chem chemical chromatography CO2H collection column combination combinatorial chemistry combinatorial libraries components compounds concentration confirmation containing decoded designed detection determined drug ELSD error example experimental Figure final flow four fractions high throughput HPLC identified increase individual initial injection ionization mass spectral mass spectrometer material methods molecular molecules observed obtained optimization overall parallel peak performance phase plate positive possible prepared present problem purification purity quantity racks range Rapid reaction reagent response sample screening selected separation shown shows single solvent sort spectra Spectrom standard step structures synthesis synthons Table techniques test tubes trace typically weight yield
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