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.