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 vi
... Preparation Methods for ESI-MS Analysis of Drugs Bound to Resin Beads 4.1 Sample Preparation Experimental Methods 4.2 Sample Preparation Results and Discussion 41 42 45 47 48 50 51 55 55 55 57 59 59 61 62 65 67 70 70 70 73 74 Contents 5 ...
... Preparation Methods for ESI-MS Analysis of Drugs Bound to Resin Beads 4.1 Sample Preparation Experimental Methods 4.2 Sample Preparation Results and Discussion 41 42 45 47 48 50 51 55 55 55 57 59 59 61 62 65 67 70 70 70 73 74 Contents 5 ...
Page 2
... prepared in 200-fold redundancy contains 10 million beads. Depending on the resin (bead) loading and the overall yield of the synthetic sequence, each bead in the library possesses ≤ 1 nmol of compound and 1–5 pmol of associated tags ...
... prepared in 200-fold redundancy contains 10 million beads. Depending on the resin (bead) loading and the overall yield of the synthetic sequence, each bead in the library possesses ≤ 1 nmol of compound and 1–5 pmol of associated tags ...
Page 3
... prepared by parallel synthesis typically provide a manageable number of compounds (<5000) in sufficient quantity (>0.1 mg) to allow identity, purity, and yield for all members (or a statistically relevant number) to be determined ...
... prepared by parallel synthesis typically provide a manageable number of compounds (<5000) in sufficient quantity (>0.1 mg) to allow identity, purity, and yield for all members (or a statistically relevant number) to be determined ...
Page 9
... sampling of 7.6%. Given that the library was prepared in 200-fold redundancy, a number of replicate structures are expected o run-1 run-2 run-3 Figure 1.4 (a) Composite library 1. High Throughput Analysis of Combinatorial Libraries Encoded ...
... sampling of 7.6%. Given that the library was prepared in 200-fold redundancy, a number of replicate structures are expected o run-1 run-2 run-3 Figure 1.4 (a) Composite library 1. High Throughput Analysis of Combinatorial Libraries Encoded ...
Page 21
... synthesize individual analogs, or prepare a follow-up optimization library. In any event, the decision regarding the design and synthesis of new compounds, will, in part, rely. High Throughput Analysis of Combinatorial Libraries Encoded 21.
... synthesize individual analogs, or prepare a follow-up optimization library. In any event, the decision regarding the design and synthesis of new compounds, will, in part, rely. High Throughput Analysis of Combinatorial Libraries Encoded 21.
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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