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 2
... overall yield of the synthetic sequence, each bead in the library possesses ≤ 1 nmol of compound and 1–5 pmol of ... overall success of the synthesis and the performance of individual synthons. With the primary goal of assessing the ...
... overall yield of the synthetic sequence, each bead in the library possesses ≤ 1 nmol of compound and 1–5 pmol of ... overall success of the synthesis and the performance of individual synthons. With the primary goal of assessing the ...
Page 3
... overall library yield and purity. Tag QC: Tag fidelity confirmed after each tagging step prior to pooling or direct divide. Construction-in-process QC: Resynthesis of 2–3 QC compounds during actual library construction using bulk ...
... overall library yield and purity. Tag QC: Tag fidelity confirmed after each tagging step prior to pooling or direct divide. Construction-in-process QC: Resynthesis of 2–3 QC compounds during actual library construction using bulk ...
Page 4
... overall success of the solid-phase synthesis and to assess the performance of each synthon. Tag decodes reveal, which compounds (synthons) are supposed to be on each bead, and LC/MS analysis reveals whether they are physically present ...
... overall success of the solid-phase synthesis and to assess the performance of each synthon. Tag decodes reveal, which compounds (synthons) are supposed to be on each bead, and LC/MS analysis reveals whether they are physically present ...
Page 12
... overall performance of the hydrophobic synthons and a higher confirmation rate of lipophilic compounds may be in part due High Throughput Analysis of Combinatorial Libraries Encoded 13 Asynthon Figure 12 I. Henderson et al.
... overall performance of the hydrophobic synthons and a higher confirmation rate of lipophilic compounds may be in part due High Throughput Analysis of Combinatorial Libraries Encoded 13 Asynthon Figure 12 I. Henderson et al.
Page 18
... Overall, sub-library 8j appeared more active and selective against cat D than plm II. Only those wells (single beads) that showed activity equal to or less than 30% of control activity remaining were decoded. This follow-up evaluation ...
... Overall, sub-library 8j appeared more active and selective against cat D than plm II. Only those wells (single beads) that showed activity equal to or less than 30% of control activity remaining were decoded. This follow-up evaluation ...
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
Popular passages
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