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The Organic Chemistry of Drug Design and Drug Action, Third Edition

By

Richard B. Silverman Ph.D , Mark W. Holladay

Description

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-π 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

Reviews

“A textbook for a semester course in medicinal chemistry for senior or first-year graduate students of chemistry or biochemistry. Approaches the subject, not from the usual perspective of classes of drugs, but by the organic chemical mechanisms and effect desired when designing new drugs” –. Annotation c. Book News, Inc., Portland, OR (booknews.com)
“Sliverman continues to blur the edges between chemistry and pharmacology in a manner that is incontrovertibly relevant to the discipline of drug design and development.”
-Michael E. Cooper, GE Healthcare, The Maynard Centre, in DDT, VOL. 9, 2004

“What stands out in comparison with other books discussed here is that the subjects are generally addressed in detail, and each theoretical point is illustrated with examples of specific drugs.”
-ORGANIC CHEMISTRY ORG., 2005

“…this book is a thorough overview of drug discovery and development… It is not only an excellent textbook for students but also a valuable resource for those already practicing medicinal chemistry.”

–JOURNAL OF MEDICINAL CHEMISTRY

“This book is a tour de force…appropriate for advanced undergraduate students and graduate students…strongly recommended to scientists who are seeking an efficient introduction to medicinal chemistry, background in a specific drug principle or category, or a dose of inspiration.”
–JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

“… unified, well-organized and clearly presented…My congratulations to Dr. Silverman in consolidating such a multiplicity of facts and data …”
–Carl Kaiser, Director of Medicinal Chemistry, NOVA PHARMACEUTICAL CORPORATION

“The author shows an uncanny ability to present the salient principles in a systematic, well-balanced and logical way…”
–William C. Groutas, Wichita State University

“…The organization of this book and the clarity of presentation are outstanding…It is highly recommended…”
–JOURNAL OF MEDICINAL CHEMISTRY

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