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Bioisosteres in Medicinal Chemistry: 54 (Methods and Principles in Medicinal Chemistry) [Hardcover]

Nathan Brown , Raimund Mannhold , Hugo Kubinyi , Gerd Folkers

RRP: 105.00
Price: 96.78 & FREE Delivery in the UK. Details
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Book Description

22 Aug 2012 3527330151 978-3527330157 1
Written with the practicing medicinal chemist in mind, this is the first modern handbook to systematically address the topic of bioisosterism. As such, it provides a ready reference on the principles and methods of bioisosteric replacement as a key tool in preclinical drug development. 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. In the final part, several real–world examples of bioisosterism in drug discovery projects are discussed. 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.

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“In all, I believe this book is a musthave handbook on bioisosteres. It is highly valuable both as a text book for graduate students and as a book of reference for the medicinal chemist working in the industry as well as in an academic setting.”  ( ChemMedChem , 1 July 2013)

From the Back Cover

Written with the practicing medicinal chemist in mind, this is the first modern handbook to systematically address the topic of bioisosterism. As such, it provides a ready reference on the principles and methods of bioisosteric replacement as a key tool in preclinical drug development. 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. In the final part, several real–world examples of bioisosterism in drug discovery projects are discussed. 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.

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Front Cover | Copyright | Table of Contents | Excerpt | Index
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