We use cookies to enhance your experience on our website. By continuing to use our website, you are agreeing to our use of cookies. You can change your cookie settings at any time. Find out more

Top Drugs

Top Synthetic Routes

John Saunders

Publication Date - 12 July 2012

ISBN: 9780198501008

96 pages


Today's top selling drugs have been uncovered from two major sources: natural products and laboratory synthesis. Those synthesised directly by medicinal chemists usually have been the result of a protracted discovery programme using a natural product (e.g. a hormone or an enzyme substrate) or a screening lead as a starting point. Many of the major categories of human disease cardiovascular, gastrointestinal, central nervous system, inflammatory and infectious diseases are included. After a short introduction to the discovery and mechanism of action of each drug, the syntheses of the best selling drugs are reviewed. Where the information exists in the literature, the original research method to each drug is compared with more recent approaches which aim either at improving the route or at validating newer methodologies or reagents in the context of drug synthesis. Since, for many drugs, the marketed product was originally prepared as a racemic mixture, perhaps the most important comparison is between that route and alternatives which involve some element of asymmetric synthesis.


  • Shows how the organic chemistry taught at undergraduate level is applied by medicinal chemists in industry
  • Enables students to see the importance of stereospecific syntheses and see how advances from academia have revolutionised the pharmaceutical industry
  • Explains how an understanding of modern organic chemistry is pivotal to the overall drug discovery process
  • Encourages students to search other more detailed texts


"This is a good introduction to the synthetic chemistry required to fuel the pharmaceutical industry and should encourage students to pursue a career in this exciting field." -- Doody's

Table of Contents

    1. Inhibitors of angiotensin converting enzyme as effective antihypertensive agents
    2. Blockade of angiotensin-II receptors
    3. Calcium channel blockers in the treatment of angina and hypertension
    4. Antagonists of histamine receptors (H2) as anti-ulcer remedies
    5. Proton pump inhibitors as gastric acid secretion inhibitors
    6. Modulation of central serotonin in the treatment of depression
    7. Hypnotic, anxiolytic, anticonvulsant and muscle relaxant agents: ligands for benzodiazepine receptors
    8. Another histamine receptor: blockers of the H[1 receptor for the treatment of seasonal allergic rhinitis
    9. Nucleoside analogues which inhibit HIV reverse transcriptase
    10. Quinolones as anti-bacterial DNA gyrase inhibitors

Related Titles