History and Development of Medicinal Chemistry, Unit-I B.Pharmacy 4th Semester Note PDF

  • Introduction to Medicinal Chemistry
  • History and development of medicinal chemistry
  • Physicochemical properties in relation to biological action
  • Ionization, Solubility, Partition Coefficient, Hydrogen bonding, Protein binding, Chelation, Bioisosterism, Optical and Geometrical isomerism.
  • Drug metabolisam
  • Drug metabolism principles- Phase I and Phase II. 
  • Factors affecting drug metabolism including stereo chemical aspects


  • Introduction to Medicinal Chemistry

    History and Development of Medicinal Chemistry

    3500 BC - Sumerians reported use of opium
    3000 BC - Chinese reported use of ephedra (Ma Huang)
    1793 - Faureroy and Vauquehin established the Ecole Supurieure de Pharmacie i.e. first to incorporate chemistry into pharmacy curriculum.
    1803 - Derosome isolated a salt from opium
    1817 - Serturner demonstrated the alkaline nature of opium
    1818 - Meissner proposed the term alkaloids
    1820 - Isolation of morphine quinine and atropine
    1842 - onwards general anesthetics were introduced, antiseptics like iodine and phenol were used in surgery
    1853 - Hennery proposed the relationship between the functional groups, modifiers and their reactivities.
    1875 - Carl buss isolated salisylic acid from Spirea ulmaria
    1884 - Phenazone was synthesized, local anesthetic action of cocaine was reported
    1890 - Hoffman named acetyl salicylic acid as aspirin
    1892 - Benzocaine was obtained by structural modification of cocaine
    1894 - Ehrlich reported lock and key theory
    1899 - 1901 - Meyer and overton related distribution coefficient with biological activity
    1910 - Barger and dale examined the response of various tissues to muscarine and nicotine
    1911 - Barbiturates were introduced as sedative
    1920 - 1930 - Identification of vitamin deficiency diseases and elucidation of structure of various vitamins
    1930 - Structure of steroid hormones
    1926 - 1946 - Synthetic antimalarial like chloroquine were introduced as a substitute of quinine
    1935 - Domagk observed antibacterial activity of sulphonamide dye stuff (prontocil red)
    1940 - Florey and Heaton isolated benzyl penicillin
    1944 -1949 - Isolation of antibiotics e.g. streptomycin, chloramphenicol and tetracyclines
    1950 -1960 - Semisynthetic corticosteroids like prednisolone and betamethasone were prepared

    Highlights of some discovered drugs

    • Morphine was isolated from opium by the German Pharmacist Sertuner in 1806, which marked the introduction of chemically pure active constituents into modem therapeutics.
    • Mydriatics base atropine introduced by Mein, Geiger and Hesse in 1833.
    • Davy (1778-1829) introduced nitrous oxide (laughing gas) as an inhalation anaesthetic and this was followed by the first clinical experiments with ether in the surgical amphitheater. Perhaps the most beneficial medicinal innovation of the nineteenth century was the discovery of general anesthesia.
    • In the two decades 1880-1900 Antipyrine introduced by Knorr (1883).
    • Aspirin introduced by Dreser's in 1889.
    • Barbital were innovated by Emil Fischer and Mering in 1903.
    • Stolz synthesized the first hormone epinephrine (Adrenaline, 1904).
    • Barger and Dale in 1909 made a fundamental study of the effect of chemical structure in the series of Sympathomimetic amines on the physiological effect of these compounds.

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