As such, it provides a ready reference on the principles and methods of bioisosteric replacement as a key tool in preclinical drug development
In the final part, several real-world examples of bioisosterism in drug discovery projects are discussed
The first part provides an overview of bioisosterism, classical bioisosteres and typical molecular interactions that need to be considered, while the second part describes a number of molecular databases as sources of bioisosteric identification and rationalization
The third part covers the four key methodologies for bioisostere identification and replacement physicochemical properties, topology, shape, and overlays of protein-ligand crystal structures
With its detailed descriptions of databases, methods and real-life case studies, this is tailor-made for busy industrial researchers with little time for reading, while remaining easily accessible to novice drug developers due to its systematic structure and introductory section.