High Throughput-Screening in Drug Discovery describes the application of parallel synthesis to lead optimization and the design and synthesis of targeted libraries. Features:

• Describes parallel synthesis approaches in combination with structure-based design of molecules that inhibit protein-protein interactions
• Covers the expansion of medicinal chemistry design concepts in the synthesis of HIV reverse transcription inhibitors
• Explores the development of novel ALK inhibitors and the melanocortin receptor agonists
• Elucidates the use of L- and D-amino acids for the synthesis of anticancer, antiviral, and anti-inflammatory compounds
• Explains the optimization of peptides, natural products, and glycoconjugates for a range of targets
• Discusses the synthesis of nucleotide-based libraries as potential antibiotics
• Illustrates several synthetic approaches for the efficient use and effective synthesis of focused libraries using parallel synthesis

Contents

1. Introduction and Review
2. Application of Parallel Synthesis to the Optimization of Inhibitors of the ZipA-FtsZ Protein-Protein Interaction
3. Case Studies of Parallel Synthesis in Hit Identification, Hit Exploration, Hit-to-Lead, and Lead Optimization Programs
4. A Successful Application of Parallel Synthesis to Computer-Assisted Structural Optimization of New Leads Targeting Human Immunodeficiency Virus-1 Reverse Transcriptase: The Case of Acylthiocarbamates and Thiocarbamates
5. How High-Throughput Medicinal Chemistry Can Expedite Lead Discovery, Lead Optimization
6. Rapid Lead Identification of Inhibitors of Adenine Nucleotide Translocase: A Case Study of Applying Combinatorial Chemistry Techniques in Drug Discovery
7. Parallel Synthesis of Anticancer, Antiinflammatory, and Antiviral Agents Derived from L-and D-Amino Acids
8. Application of Solid-Phase Parallel Synthesis in Lead Optimization Studies
9. High-Throughput Solid-Phase Synthesis of Nucleoside-Based Libraries in the Search for New Antibiotics

Index

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