Privileged Scaffolds in Medicinal Chemistry: Design, Synthesis, Evaluation

By Stefan Braese (Editor), Ana Martinez (Editor), Stefan Brase (Editor), Dorota Jakubczyk (Contribution by), Roland Pfau (Contribution by), Arantxa Encinas (Contribution by), Esther Rosch (Contribution by), Carmen Gil (Contribution by), Kye Masters (Contribution by), Franziska Glaser (Contribution by), Carsten S Kramer (Contribution by), David Newman (Contribution by), Frederico Albericio (Contribution by), Henning Steinhagen (Contribution by), Lucija Peterlin Masic (Contribution by), Shahriar Mobashery (Contribution by), Eliezer J Barreiro (Contribution by), Wolfgang Wenzel (Contribution by), Mayland Chang (Contribution by), David Thurston (Editor in chief)
One strategy to expedite the discovery of new drugs, a process that is somewhat slow and serendipitous, is the identification and use of privileged scaffolds. This book covers the history of the discovery and use of privileged scaffolds and addresses the various classes of these important molecular fragments.
The first of the benzodiazepines, a class of drugs that is powerful for treating anxiety, may not have been discovered had it not been for a chance experiment on the contents of a discarded flask found during a lab clean-up. Some years later, scientists discovered that benzodiazepine derivatives were also effective in treating other diseases. This class of molecules was the first to be described as privileged in the sense that it is especially effective at altering the course of disease. Other privileged molecular structures have since been discovered, and since these compounds are so effective at interacting with numerous classes of proteins, they may be an effective starting point to look for new drugs against the supposedly “undruggable” proteins.
Following introductory chapters presenting an overview, a historical perspective and the theoretical background and findings, main chapters describe the structure of privileged structures in turn and discuss major drug classes associated with them and their syntheses. This book provides comprehensive coverage of the subject through chapters contributed by expert authors from both academia and industry and will be an excellent reference source for medicinal chemists of a range of disciplines and experiences.

Privileged scaffolds in medicinal chemistry: An introduction; Privileged scaffolds in medicinal chemistry: A computational approach; The beta-Lactam (Azetidin-2-one) as a privileged ring in medicinal chemistry; (Benz)imidazoles; Pyrazoles; Quinolones: Privileged scaffolds in medicinal chemistry; Isoquinolines; Rhodanine; Heterocycles containinf nitrogen and sulfur as potent biologically active scaffolds; Thiirane class of gelatinase inhibitors as a privileged tempate that cross the blood-brain barrier; Coumarins; Xanthones are privileged scaffolds in medicinal chemistry - but are they over privileged?; Natural product scaffolds of value in medicinal chemistry; Ergot alkaloids; Cyclic Peptides as Privileged structures; Spirocycles as privileged structural motifs in medicinal chemistry;
This book addresses the various classes of privileged scaffolds and covers the history of their discovery and use.


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About the Hardcover

Publisher Royal Society of Chemistry
Publish date 09/30/2015
Pages 476
ISBN-13 9781782620303
Language English