_The Organic Chemistry of Drug Design and Drug Action, Third Edition_,
represents a unique approach to medicinal chemistry based on physical
organic chemical principles and reaction mechanisms that rationalize
drug action, which allows the reader to extrapolate those core
principles and mechanisms to many related classes of drug molecules.
This new edition reflects significant changes in the process of drug
design over the last decade. It preserves the successful approach of
the previous editions while including significant changes in format
and coverage.
New to this edition:
* Updates to all chapters, including new examples and references
* Chapter 1 (Introduction): Completely rewritten and expanded as an
overview of topics discussed in detail throughout the book
* Chapter 2 (Lead Discovery and Lead Modification): Sections on
sources of compounds for screening including library collections,
virtual screening, and computational methods, as well as hit-to-lead
and scaffold hopping; expanded sections on sources of lead compounds,
fragment-based lead discovery, and molecular graphics; and
deemphasized solid-phase synthesis and combinatorial chemistry
* Chapter 3 (Receptors): Drug-receptor interactions, cation-p and
halogen bonding; atropisomers; case history of the insomnia drug
suvorexant
* Chapter 4 (Enzymes): Expanded sections on enzyme catalysis in drug
discovery and enzyme synthesis
* Chapter 5 (Enzyme Inhibition and Inactivation): New case histories:
* for competitive inhibition, the epidermal growth factor receptor
tyrosine kinase inhibitor, erlotinib and Abelson kinase inhibitor,
imatinib
* for transition state analogue inhibition, the purine nucleoside
phosphorylase inhibitors, forodesine and DADMe-ImmH, as well as the
mechanism of the multisubstrate analog inhibitor isoniazid
* for slow, tight-binding inhibition, the dipeptidyl peptidase-4
inhibitor, saxagliptin
* Chapter 7 (Drug Resistance and Drug Synergism): This new chapter
includes topics taken from two chapters in the previous edition, with
many new examples
* Chapter 8 (Drug Metabolism): Discussions of toxicophores and
reactive metabolites
* Chapter 9 (Prodrugs and Drug Delivery Systems): Discussion of
antibody–drug conjugates
Les mer
Produktdetaljer
ISBN
9780123820303
Publisert
2014
Utgave
3. utgave
Utgiver
Vendor
Academic Press
Språk
Product language
Engelsk
Format
Product format
Digital bok
Forfatter