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The Evolution of Drug Discovery

ISBN: 978-3-527-32669-3
528 pages
April 2011
The Evolution of Drug Discovery (3527326693) cover image
The discovery and use of medicines is just as fascinating a human scientific endeavor as space flight or the tracing of human evolution. It is also the everyday task of hundreds of thousands of pharmacists, pharmaceutical chemists and researchers worldwide.
Based on his profound knowledge of past and present paradigms in the development of medicines, Enrique Ravina takes the reader from the very beginnings of pharmacology to the multibillion-dollar business it represents today. Recounting the often spectacular successes and failures of innovative drugs as well as the people who discovered them, he brings abstract science to life in anecdotal form.
For anyone with a more than superficial interest in the science of drugs and all those interested in knowing how drugs have been developed, how they have reached us, and became part of our daily life. This book is beautifully illustrated, containing many rare and historical photographs of drugs and their discoverers, and abounds with references to the primary literature, listing seminal publications alongside more modern reviews for readers seeking further details.

With a Foreword by Hugo Kubinyi
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Foreword
Preface and Acknowledgment

EVOLUTION OF DRUG DISCOVERY
Antiquity
Great Periods of Drug Discovery
Vaccines

THE FIRST SYNTHETIC DRUGS AND THE BIRTH OF CHEMOTHERAPY
Aspirin, Phenacetin, and Paracetamol
Discovery of Pyrazolones
Cocaine and Local Anesthetics
Barbiturates and Related Compounds
Fathers of Chemotherapy

FROM CASUAL OBSERVATIONS TO SYSTEMATIC SEARCH
From Antihistamines to Antipsychotics and Antidepressants: The Origins of Psychopharmacology
Benzodiazepines
Structural Variations on Sulfanilamide
Azoles as a Source of Antibacterials, Antifungals, and Antihelmintics
The Long Fight Against Cancer
Sildenafil -
The First Inhibitor of Rectile Dysfunction

NATURE AS A SOURCE OF DRUGS: DRUGS FROM NATURAL PRODUCTS
Plant Sources: Derivatives and Related Drugs (Selected Examples)
Animal Sources: Derivatives and Related Drugs
Drugs from Microbiological Sources
Drugs from Marine Origin: The Contribution of the Sea to the Therapeutic Arsenal

RATIONALIZING THE DRUG DISCOVERY PROCESS
Early Rational Drug Discovery Approaches: L-Dopa and L-Alpha-Methyldopa
Receptor-Based Drug Discovery
Antimetabolites in the Fight Against Bacteria, Viruses, and Cancer
Cyclooxygenase(COX) Inhibitors

STRUCTURE-BASED DRUG DISCOVERY
Searching for the Ideal Antihypertensive Agent: Renin-Angiotensin-Aldosterone System (RAAS)
HIV Protease Inhibitors
Drugs Effective Against the Influenza Virus (the Flu)
Fight Against Cancer
New Avenues for the Development of Antidiabetic Agents. Dipeptidyl-Peptidase-IV Inhibitors: Sitagliptin and Vildaglptin

BIOPHARMACEUTICALS
Monoclonal Antibodies (MAbs)
Recombinant DNA Technology (Genetic Engineering)
Some Recombinant Protein Drugs
Protein-Polyethyleneglycol (PEG) Conjugates (Protein PEGylation)

DRUG DISCOVERY IN THE POSTGENOMIC ERA: CONCLUDING REMARKS
Chemical/Genomic Strategy
Summary
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Enrique Raviņa studied pharmacy at the University of Santiago de Compostela, Spain, where he obtained his PhD in 1969 and was appointed Professor of Organic Chemistry in 1975. Since 1981 he is Professor of Medicinal/Pharmaceutical Chemistry at the same University. He is a member of the Spanish Royal Academy of Pharmacy, a founding member of the Spanish Society of Medicinal Chemistry and a member of the American Chemical Society. Professor Raviņa has over 120 publications to his name in the field of chemistry of drugs, especially in the area of antipsychotic and cardiovascular potential drugs, including a book, book chapters, as well as a co-inventor of the world patent "6-phenyldihydropyrrolopyrimidinedione derivatives".
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"This serves as an excellent companion to many of the popular medicinal chemistry and pharmacology books, and gives students additional insight into the contemporary drug discovery process." (Doody's, 16 March 2012)

"The text is well referenced and complete with chemical illustrations. . . Recommended. Upper-division undergraduates through professionals." (Choice, 1 October 2011)

"It can be used by students interested in the classic achievements and case stories of drug discovery, but also by more experienced scientists as a guiding overview on the field. Last but not least, it serves well as a compendium to industrial professionals in the field of biomedical and medicinal chemistry research." (ChemMedChem, 2011)

 

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