High-Throughput Lead Optimization in Drug Discovery: Critical Reviews in Combinatorial Chemistry
Editat de Tushar Kshirsagaren Limba Engleză Paperback – 25 sep 2019
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. It includes more than 15 case studies that encompass a range of biological targets for application in different therapeutic areas. The text contains examples of solid and solution-phase techniques for the synthesis of directed libraries. The chapter authors explain the design principles they used to direct the choice of templates and diversity elements.
Speed Up Drug Discovery and the Hit-to-Lead Process
Focusing on the application of combinatorial chemistry to medicinal chemistry, this volume compiles a series of optimization projects that give you a snapshot of successes and challenges in the use of parallel synthesis for lead optimization. It explores how this technology, when applied to library design, can speed up drug discovery.
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Specificații
ISBN-13: 9780367387716
ISBN-10: 0367387719
Pagini: 256
Dimensiuni: 178 x 254 x 15 mm
Greutate: 0.5 kg
Ediția:1
Editura: CRC Press
Colecția CRC Press
Seria Critical Reviews in Combinatorial Chemistry
Locul publicării:Boca Raton, United States
ISBN-10: 0367387719
Pagini: 256
Dimensiuni: 178 x 254 x 15 mm
Greutate: 0.5 kg
Ediția:1
Editura: CRC Press
Colecția CRC Press
Seria Critical Reviews in Combinatorial Chemistry
Locul publicării:Boca Raton, United States
Public țintă
Academic and Professional Practice & DevelopmentCuprins
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.
Recenzii
"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
– Jan W. F. Wasley, Simpharma LLC, in Journal of Medicinal Chemistry, 2008, Vol. 51, No. 23
Descriere
A single source on parallel synthesis for lead optimization, this book features real-world examples and contributions from well-known scientists. It explores the shift to conducting parallel lead optimization in-house while outsourcing most of the screening libraries synthesis. With more than 15 case studies that encompass a range of biological targets for application in different therapeutic areas, the text contains examples of solid and solution-phase techniques for the synthesis of directed libraries. The authors explain the design principles they used to direct the choice of templates and diversity elements and they explore how this technology, when applied to library design, can speed up drug discovery.