2. INTRODUCTION
• Medicinal chemistry involves all the aspects of biological, medical and pharmaceutical
science.
• It is concerned with the invention, discovery, design, identification, preparation of biologically
active compounds.
• It involves the interpretation of their mode of action at the molecular level and the-
construction of structure-activity relationships (SARs).
• It is an important branch of chemistry which is directly related to health care with branches of
chemistry like organic, inorganic, biochemistry and analytical chemistry.
3. • According to recommendations of International Union of Pure And Applied Chemist" (IUPAC) "it concerns
with the discovery, the development, the identification of the mode of action of biologically active
compounds at the molecular level". It involves-Synthesis,SAR,Receptor Interactions and Absorption,
Distribution, Metabolism and Excretion
• Medicinal Chemistry concerns with the understanding of mechanisms of action of drugs,means
it involves the isolation, characterization and synthesis of compounds that can be used in
medicine for the prevention, treatment, and cure of disease.
• It describes the functional groups present in the drug and their relation to the rest of the
molecule. This helps us to know which part of molecule contributes to the medicinal effects
and suitable alterations is to be done for better effect.
4. HISTORY AND DEVELOPMENT
• In history a large number of plants Were used to treat various diseases. The uses of plants were described and were recorded
in the writings of Hippocrates, Galenous and Dioscorides.
• Greek Physician, Hippocartes (450 B.C.), laid the foundation of modern medicine.
• In India later on, a large number of medicinal preparations including AYURVEDA
• were described by physicians such as CHARAK, ISUSHRUTÅ.
• The scholar Emperor Shen Nung (2735 B.C) compiled a book of herbs.
Shen Nung
Hippocartes
5. The 19th century is regarded as the birth period of modern medicinal chemistry with the invention of
different active metabolites or simply the medicines
History and Development can be summarized as
1. 3500 BC — Sumerians reported use of opium 2. 3000 BC — Chinese reported use of ephedra (Eda Huang)
3. 1793 - Faureroy and Vauquehin established thé Ecole Supurieure de Pharmacie i.e. first to
incorporate chemistry into pharmacy curriculum
4. 1803 Derosome isolated a salt from opium 5.1820 — Isolation of morphine, quinine and atropine
6. 1842 — onwards general anesthetics were introduced, antiseptics like iodine and phenol were used in surgery
6. 7. 1875 — Carl buss isolated salicylic acid from Spirea ulmaria 8. 1890 — Hoffman named acetyl salicylic acid as aspirin
9. 1894 — Ehrlich reported lock and key theory
10. 1911 Barbiturates were introduced as sedatives 11.1930— Structure of steroid hormones
7. 12 1926 — 1946 — Synthetic antimalarials like chloroquine were introduced as a substitute of quinine
13. 1935 — Domagk observed antibacterial activity of sulphonamide dye stuff (prontocil red)
14. 1940 — Florey and Heaton isolated benzyl penicillin
15.1944 -1949 – Isolation of antibiotics e.g. streptomycin, chloramphenicol and tetracycline
16. 1950-60 — Semisynthetic corticosteroids like prednisolone and betamethasone were-prepared.
