Main description:

Drug Discovery with Privileged Building Blocks traces back PharmaBlock's founding philosophy of designing privileged building blocks. High-quality building blocks are crucial not only to biological activities of different molecules but also to ADMET properties, which eventually will impact the success rate of drug discovery projects. A thorough study of how building blocks perform in drug molecules and a regular analysis of new building block structures in the latest researches have proven to be a fruitful strategy to generate novel building blocks. Using this strategy, PharmaBlock has supplied the drug industry with a great number of building blocks, which are increasingly being adopted by drug hunters, and these are identified in this book.

Each chapter may be read and studied without learning the previous chapters. This book will be a good starting point for novice medicinal chemists, and veteran medicinal chemists will find it useful as well.

Key Feature

The book covers privileged building blocks appearing most frequently on patents for novel drugs.

The latest relevant tactics are explained in the context of drug design and medicinal chemistry.

Key synthesis, especially large-scale synthesis, is described.

The most recent literature references are cited.

Contents:

Preface 1. Alkynes; 2. Azaindoles; 3. Azetidines; 4. Bicyclic Pyridines Containing Ring-junction N; 5. Bicyclo (1.1.1)pentyl (BCP) as an sp3 Carbon-rich Bioisostere for para-Phenyl and tert-Butyl Groups; 6. Bicyclo[2.2.2]octane (BCO) as A 3D-rich Bioisotere for the para-Phenyl Group; 7. Bicyclo[3.1.0]hexanes; 8. Bridge-Fused Rings as m-Phenyl Bioisosteres; 9. Cubanes, Are We There Yet?; 10. Cyclobutanes; 11. Cyclohexanes; 12. Cyclopentanes; 13. Cyclopropanes as Metabolically More Robust Bioisoteres for Linear Alkyl Substituents; 14. Deazapurines; 15. Furopyridines; 16. Indazoles; 17. Indoles; 18. Oxetanes; 19. Piperidine, the Enchanted Ring; 20. Pyrazines; 21. Pyrazoles; 22. Pyridazines; 23. Pyridines - The Magic of Phenyl-Pyridyl Switch; 24. Pyrimidines; 25. Pyrrolidines; 26. Pyrrolotriazines; 27. Spiroazetidines; 28. Spirocyclic Piperidines; 29. Spirocyclic pyrrolidines; 30. Spirooxetanes; 31. Tetrahydropyrans; 32. Trifluoromethylpyridines. Index