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MAKROZYKLEN IN DER DROGENENTDECKU
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eBay-Artikelnr.:226087040551
Artikelmerkmale
- Artikelzustand
- ISBN-10
- 1849737010
- Book Title
- Macrocycles in Drug Discovery (Drug Discovery (Volume 40))
- Genre
- MEDICAL
- Item Height
- 9.25 inches
- ISBN
- 9781849737012
- Publication Year
- 2014
- Series
- Issn Ser.
- Type
- Textbook
- Format
- Hardcover
- Language
- English
- Publication Name
- Macrocycles in Drug Discovery
- Item Length
- 9.2in
- Publisher
- Royal Society of Real Chemistry, T.H.E.
- Item Width
- 6.1in
- Item Weight
- 33.1 Oz
- Number of Pages
- 528 Pages
Über dieses Produkt
Product Information
This book reviews macrocycles in drug discovery, both those of natural origin and semi-synthetic derivatives of natural products, and those designed and synthesized based on principles of medicinal chemistry. The medicinal chemistry of macrocyclic natural products is interesting in itself, but lessons learned from these compounds, in terms of the relationship between structure and desirable physicochemical properties, are now informing the design of fully synthetic macrocyclic drug candidates against a variety of targets including kinases, ATPases, proteases, GPCRs and others. Furthermore, as more non-classical drug targets, such as protein-protein interactions, are pursued in the pharmaceutical industry, macrocyclic molecules are generating increasing interest as they offer a way to provide drug-protein interactions that cover a larger surface area than traditional small molecules. A variety of macrocycles have become important drugs or have been identified as leads to marketed drugs. This text will discuss these compounds, their pharmacology and synthesis, in the context of their broad chemotype as compounds composed of large rings. Providing a wide reaching review of this important area in a single volume, this book will be of interest to biochemists, pharmaceutical scientists and medicinal chemists working in industry or academia.
Product Identifiers
Publisher
Royal Society of Real Chemistry, T.H.E.
ISBN-10
1849737010
ISBN-13
9781849737012
eBay Product ID (ePID)
201617975
Product Key Features
Publication Name
Macrocycles in Drug Discovery
Format
Hardcover
Language
English
Publication Year
2014
Series
Issn Ser.
Type
Textbook
Number of Pages
528 Pages
Dimensions
Item Length
9.2in
Item Width
6.1in
Item Weight
33.1 Oz
Additional Product Features
Series Volume Number
Volume 40
Lc Classification Number
Qd400
Reviews
""Macrocycles in Drug Discovery" provides an in-depth review with case studies of some of the major targets and areas that have been the focus of macro- cyclic drug discovery. It also provides useful insights into macrocycle cell permeability, oral bioavailability and methods for their synthesis." "...rich in information..." "I absolutely recommend "Macrocycles in Drug Discovery" to those that are active in the field, both in academia and the pharmaceutical industry. The different chapters provide stimulating reading for experts in macrocycles as well as for organic chemists and medicinal chemists in general. The comprehensive chapters also serve as a source of references with extensive citation of the primary literature.", "The book is a wellmade snapshot of current research, describing development stories of established macrocycle drugs and their properties, as well as new avenues in their development." "The book's 11 chapters, written by distinguished experts, are mostly dedicated to macrocycles for a specific protein target or target class." "Numerous examples presented along with the compounds' potency, selectivity, permeability, bioavailability and other properties allow the reader to understand which determinants make a successful macrocyclic drug.", Macrocycles are ring-shaped molecules containing12 or more ring atoms. Many important drugs belong to this structural class, for example the immunosuppressant cyclosporine or the antibiotic vancomycin. Macrocycles' ability to bind difficult targets that are considered 'undruggable' by traditional small molecule drugs has produced much interest. Recent innovations for designing de novo macrocycles and for screening large combinatorial macrocycle libraries have given an additional impulse to the field's development. The book is a well-made snapshot of current research, describing development stories of established macrocycle drugs and their properties, as well as new avenues in their development. The book's 11chapters, written by distinguished experts, are mostly dedicated to macrocycles for a specific protein target or target class. The targets discussed include heat shock protein, tubulin, histone deacetylases, kinases, proteases, G-protein coupled receptors, integrins, and protein protein interactions. Several authors provide introductory sections about the general characteristics of macrocycles, meaning that there is a small overlap between some chapters. However, this is not negative at all as it offers different perspectives on the topic. Most established macrocyclic drugs are based on natural products that were identified in bacteria, fungi, plants or other organisms. Consequently, the majority of molecules discussed are natural products or derivatives thereof. As nature does not offer macrocycles for every therapeutic target, scientists have designed new macrocycles, which are also covered in the book. Chapters are dedicated to the design of kinase inhibitors and to intriguing strategies for developing macrocycles de novo by mimicking protein epitopes such as hairpins or helices. To develop novel macrocycles, it is essential to understand the factors that affect their permeability and bioavailability-important topics that are discussed in the penultimate chapter. The book concludes with a comprehensive chapter on synthetic strategies for the production of macrocycles. In summary, this title is an in depth discussion of macrocycle drug discovery. Numerous examples presented along with the compounds' potency, selectivity, permeability, bioavailability and other properties allow the reader to understand which determinants make a successful macrocyclic drug.
Table of Content
Introduction; Bioactive Macrocycles from Nature; Recent Advances in Macrocyclic Hsp90 Inhibitors; Epothilones; Macrocyclic Inhibitors of Zinc-dependent Histone Deacetylases (HDACs); Designed Macrocyclic Kinase Inhibitors; Anti-Inflammatory Macrolides to Manage Chronic Neutrophilic Inflammation; Linear and Macrocyclic Hepatitis C Virus Protease Inhibitors; Macrocyclic Inhibitors of GPCR's, Integrins and Protein-Protein Interactions; Macrocyclic a-Helical Peptide Drug Discovery; Optimizing the Permeability and Oral Bioavailability of Macrocycles; The Synthesis of Macrocycles for Drug Discovery
Copyright Date
2015
Topic
Toxicology, Pharmacy, Pharmacology
Intended Audience
Scholarly & Professional
Illustrated
Yes
Genre
Medical
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eBay-Artikelnr.:226087040551
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