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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From inside the book
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Page 2
... synthons are serially combined through split-and-pool or direct divide” synthesis in tandem with the incorporation of binary sets of electrophoric tags on solid support. Each bead in an encoded library contains a compound, whose ...
... synthons are serially combined through split-and-pool or direct divide” synthesis in tandem with the incorporation of binary sets of electrophoric tags on solid support. Each bead in an encoded library contains a compound, whose ...
Page 3
... Synthon profiling/reaction optimization: Confirmation of reagent viability, establishing suitability of monomer ... synthons. Production-in-process QC: Production safeguard to ensure optimal elution of library compounds into essay ...
... Synthon profiling/reaction optimization: Confirmation of reagent viability, establishing suitability of monomer ... synthons. Production-in-process QC: Production safeguard to ensure optimal elution of library compounds into essay ...
Page 4
... synthons. 3 STATISTICAL CONSIDERATIONS The goals of sampling an encoded combinatorial library are to determine the overall success of the solid-phase synthesis and to assess the performance of each synthon. Tag decodes reveal, which ...
... synthons. 3 STATISTICAL CONSIDERATIONS The goals of sampling an encoded combinatorial library are to determine the overall success of the solid-phase synthesis and to assess the performance of each synthon. Tag decodes reveal, which ...
Page 5
... synthons in a library, with the proviso that the synthon sample size, nij, must be sufficiently large (> 10 ." Library QA provides no information regarding the combinatorial synthesis success of synthons or intermediates, as the ...
... synthons in a library, with the proviso that the synthon sample size, nij, must be sufficiently large (> 10 ." Library QA provides no information regarding the combinatorial synthesis success of synthons or intermediates, as the ...
Page 6
... NBOC H2N No. took H2N S. A32 A33 A34 C onco or ... H2N C| A37 A38 A39 Figure 1.3 Synthons used for statin library 1. H.NTS' SOMe A5 O A30 -O A35 Qs Fmococo H Fmochosocot Fmoc-INTNTSCO2H N -Co-H CO2H N 2 6 I. Henderson et al.
... NBOC H2N No. took H2N S. A32 A33 A34 C onco or ... H2N C| A37 A38 A39 Figure 1.3 Synthons used for statin library 1. H.NTS' SOMe A5 O A30 -O A35 Qs Fmococo H Fmochosocot Fmoc-INTNTSCO2H N -Co-H CO2H N 2 6 I. Henderson et al.
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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