Description
Book SynopsisA Single Source on Parallel Synthesis for Lead Optimization The end of the previous millennium saw an explosion in the application of parallel synthesis techniques for making compounds for high-throughput screening. Over time, it became clear that more thought in the design phase of library development is necessary to generate high quality hits. More recently, the use of parallel synthesis techniques has shifted to applications beyond screening collections. Exploring the nuances of this technology, High-Throughput Lead Optimization in Drug Discovery describes the application of parallel synthesis to lead optimization and the design and synthesis of targeted libraries.
Examine Case Studies that Cover a Range of Different Biological Targets
Featuring real-world examples and contributions from well-known scientists, the book explores the shift to conducting parallel lead optimization in-house while outsourcing most of the screening libraries synthesis.
Trade Review
"Overall, this book is a successful attempt to provide in one volume many illustrative examples in this evolving field and it presents a wealth of information on topics that demonstrate the versatility and power of the technology."
– Jan W. F. Wasley, Simpharma LLC, in Journal of Medicinal Chemistry, 2008, Vol. 51, No. 23
Table of ContentsIntroduction and Review. Application of Parallel Synthesis to the Optimization of Inhibitors of the ZipA-FtsZ Protein-Protein Interaction. Case Studies of Parallel Synthesis in Hit Identification, Hit Exploration, Hit-to-Lead, and Lead Optimization Programs. 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. How High-Throughput Medicinal Chemistry Can Expedite Lead Discovery, Lead Optimization, and Beyond. Rapid Lead Identification of Inhibitors of Adenine Nucleotide Translocase: A Case Study of Applying Combinatorial Chemistry Techniques in Drug Discovery. Parallel Synthesis of Anticancer, Antiinflammatory, and Antiviral Agents Derived from L-and D-Amino Acids. Application of Solid-Phase Parallel Synthesis in Lead Optimization Studies. High-Throughput Solid-Phase Synthesis of Nucleoside-Based Libraries in the Search for New Antibiotics.
