High-Throughput Lead Optimization in Drug Discovery

"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

• Introduction 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.