Introduction to Medicinal Chemistry
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Questions and Answers

What plant was used by the American Indians for its medicinal properties?

  • Coca Leaves
  • Ipecacuanha Root
  • Chaulmoogra Fruit (correct)
  • Opium

    • Which of these accurately describes the 19th Century in terms of medicinal chemistry?

  • The use of plants in medicine was abandoned in favor of synthesized chemical compounds.
  • The importance of chemistry in understanding drug mechanisms was completely disregarded.
  • The invention of microscopes allowed for the discovery of the active compounds within plants.
  • The focus shifted from finding new medicaments from plants, to understanding the active ingredients that caused their effects. (correct)

    • During the Middle Ages, what substance did Paracelsus believe had cure-all properties?

  • Morphine
  • Sodium Chloride (NaCl)
  • Aspirin
  • Antimony (Sb) (correct)

    • Which of these is NOT a historical example of a drug used in antiquity?

    <p>Penicillin (D)</p> Signup and view all the answers

    Which of these is the earliest recorded example of a drug used in history?

    <p>Ma huang (A)</p> Signup and view all the answers

    Which of the following drugs was discovered in the 19th century?

    <p>Quinine sulfate (C)</p> Signup and view all the answers

    What was the first mass-produced synthetic drug?

    <p>Aspirin (B)</p> Signup and view all the answers

    Which of the following is NOT a synthetic drug?

    <p>Emetine (D)</p> Signup and view all the answers

    Which of the following scientists discovered penicillin?

    <p>Alexander Fleming (A)</p> Signup and view all the answers

    Which of the following is a type of antidepressant?

    <p>Fluoxetine (C)</p> Signup and view all the answers

    Which of the following drugs was discovered during the Middle Ages?

    <p>Laudanum (D)</p> Signup and view all the answers

    What is the primary function of an SSRI drug?

    <p>To increase serotonin levels in the brain (D)</p> Signup and view all the answers

    Which of the following drugs was discovered in the early 20th century?

    <p>Insulin (A)</p> Signup and view all the answers

    Which of these drugs were not discovered in the 19th century?

    <p>Digoxin (A), Cisplatin (C)</p> Signup and view all the answers

    Which discovery or event paved the way for anticholesterol drugs?

    <p>The discovery of Compactin (Mevastin) in 1973 (B)</p> Signup and view all the answers

    Which of the following scientists discovered oxytocin?

    <p>Henry Dale (C)</p> Signup and view all the answers

    Which of the following is NOT a steroid?

    <p>Chlorpromazine (A)</p> Signup and view all the answers

    Which of the following drugs is NOT a structural analogue of cocaine?

    <p>Phenytoin (D)</p> Signup and view all the answers

    Which of the following drugs was discovered in 1963?

    <p>Paclitaxel (D)</p> Signup and view all the answers

    Which of the following drugs is an emergency contraceptive?

    <p>Levonorgestrel (C)</p> Signup and view all the answers

    Which of the following drugs is an inorganic drug?

    <p>Cisplatin (A)</p> Signup and view all the answers

    Flashcards

    Medicinal Chemistry

    The study of chemical compounds for therapeutic use in medicine.

    Quantitative Structure-Activity Relationship

    A method to predict the effects of molecular structures on biological activity.

    Morphine Extraction

    Morphine was first extracted from poppy by Serturner in 1805, revealing its properties.

    Paracelsus

    A historical figure who promoted the use of chemicals as cure-alls in medicine.

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    Chaulmoogra Fruit

    A traditional remedy used for various ailments by American Indians.

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    Laudanum

    A narcotic that induces sleep, historically used as a painkiller.

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    Phenobarbital

    A barbiturate developed from barbituric acid, used as a sedative and anticonvulsant.

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    Cocaine

    The first local anesthetic, isolated from Erythroxylon coca, used for numbing.

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    Digitalis purpurea

    A plant used for heart conditions, discovered by William Withering in 1775.

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    Compactin (Mevastatin)

    The first anticholesterol drug, discovered by Akira Endo from Penicillium citrinum in 1973.

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    6-mercaptopurine

    First effective leukemia drug developed by George Hitchings and Gertrude Elion.

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    Cisplatin

    A gold-standard drug for cancer therapy, particularly effective against testicular cancer.

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    Organic Pharmaceutical Chemistry

    The study of carbon-based drugs involving chemistry and pharmacy.

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    Emetine

    A compound isolated from Ipecacuanha by Pierre-Pelletier in 1816.

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    Quinine sulfate

    An antimalarial compound derived from Cinchona bark, produced in Pelletier's factory.

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    Acetic Acid

    A compound synthesized by Adolph Kolbe in 1845, used as a precursor in various chemical reactions.

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    Side Chain Theory

    Ehrlich's hypothesis from 1897 that the molecular structure affects a drug's effectiveness.

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    Aspirin

    The first mass-produced synthetic drug, created by Bayer in 1898.

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    Penicillin

    Discovered by Alexander Fleming in 1929, it was the first true antibiotic.

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    Chlorpromazine

    A key psychiatric treatment breakthrough, marking the start of antipsychotic drug development.

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    Insulin

    Discovered by Banting and Best in 1921, critical for diabetes management.

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    Norethindrone

    The first orally active contraceptive steroid synthesized by Carl Djerassi in 1950.

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    Mifepristone

    An abortion pill introduced in 1980, used in medical abortions.

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    Study Notes

    Introduction to Medicinal Chemistry

    • This presentation covers the history and evolution of medicinal chemistry.
    • It defines organic pharmaceutical chemistry.
    • It outlines the quantitative relationship between structure and activity.
    • It details the functional groups involved in organic chemistry.

    Drugs of Antiquity

    • Shen Nung (2735 BC) is associated with early medicinal use of plants, including Ch'ang shang and Ma huang.
    • American Indians used Chaulmoogra fruit, Ipecacuanha root, and Coca leaves.
    • The Greek Apothecary used opium, squill, hyoscyamus, viper toxin, metal ores (Cu, Zn, Fe sulfate, Cadmium oxide).

    Middle Ages

    • Chemistry and physics shifted from Greco-Roman to Arabian alchemists.
    • Paracelsus believed in using chemicals (Sb) as cures.

    19th Century: Age of Innovation and Chemistry

    • Medicine progressed from plant-derived drugs to the identification of active compounds within plants.
    • 1805 - Morphine extraction from poppies by Serturner.
    • 1810 - Hahnemann introduces homeopathy, a theory differing from Galen's approach.
    • 1816 - Emetine isolation from Ipecacuanha by Pierre-Pelletier.
    • 1820 - Caffeine, quinine, and colchicine purification.
    • 1826 - Mass production of quinine.
    • 1845 - Adolph Kolbe synthesizes Acetic Acid.
    • 1878 - John Langley proposes a biological receptor model.
    • 1886 - Coniine, an alkaloid from hemlock, synthesis.
    • 1897 - Ehrlich describes the Side Chain Theory, linking molecular structure with function.
    • 1898 - Bayer produces the synthetic drug Aspirin in mass quantities.

    20th Century and Pharmaceutical Industry

    • Synthetic chemotherapeutic agents emerge.
    • 1929 - Fleming discovers penicillin.
    • 1940 - Sulfonamide-like drugs display bacteriostatic action.
    • 1973 - Akira Endo discovers the cholesterol-lowering drug Compactin.
    • 1978 - Merck discovers a substance identical to Endo's, naming it Lovastatin.
    • Later development of statins like Atorvastatin (Lipitor).

    Psychopharmacologic Agents and Era of Brain Research

    • Chlorpromazine and Imipramine are significant psychiatric breakthroughs.
    • Iproniazid's antidepressant effects.
    • 1970s development of Tricyclic antidepressants and later of SSRI.
    • Development of benzodiazepines.

    Endocrine Therapy and Steroid

    • Epinephrine's discovery as a pure hormone.
    • 1904 - Oxytocin discovery.
    • 1914 - Thyroxine isolation.
    • 1921 - Banting and Best discover insulin.
    • Development of genetically engineered insulins (Humulin).
    • Symlin(2005) and inhaled insulin (2006) for Type 1 diabetes.
    • 1930 - Diosgenin to Progesterone Conversion.
    • Norethindrone(1950), Progesterone(1956).
    • Mifepristone(1980); Misoprostol and morning-after pill development(1994).

    Anesthetics and Analgesics

    • Historic development, from nitrous oxide to ether and chloroform, as anesthetics.
    • Horace Wells, Crawford Long, and William Morton
    • Early development of anesthetic use in medicine.

    Hypnotics and Anticonvulsants

    • Laudanum and other early sleep-inducing drugs.
    • 1864 - Von Beyer synthesizes barbituric acid.
    • Bayer introduce Phenobarbital (Luminal).
    • Development and use of Hydantoins (Phenytoin-Dilantin).

    Local Anesthetics

    • Cocaine's isolation (1860) and use in medicine.
    • 1897- Carl Koller's use for topical anesthesia.
    • Development of related compounds (Benzocaine, procaine, tetracaine, and lidocaine).

    Drugs Affecting Renal and Cardiovascular Function

    • Digitalis purpurea's discovery of its beneficial effects (1775).
    • 1841 - Digitoxin isolation.
    • 1929 - Digoxin isolation.
    • 1970s development of cholesterol-lowering drugs.

    Antineoplastic Agents

    • Sulfur mustards and nitrogen mustards and their initial use against leukemia.
    • 1893 - Cisplatin discovery.
    • 1963 - Paclitaxel (Taxol) discovery.
    • Carboplatin developed later as a second generation drug.

    Organic Pharmaceutical Chemistry

    • Focuses on developing carbon-based medicinals.
    • Combines chemistry and pharmacy.
    • Involves drug design, synthesis, and development.
    • Identifies, synthesizes, and develops chemical entities for therapeutic use.
    • Focuses on quality assurance in medicines.

    Quantitative Structure-Activity Relationship (QSAR)

    • Strategy to understand how changing a molecule's structure affects biological activity.
    • Predicts activity changes based on structural modifications.

    Functional Groups in Organic Chemistry

    • Detailed classification of functional groups and their roles in organic chemistry
    • Key examples of different functional groups, naming conventions, and structural representations.

    Hydrocarbons

    • Classification of hydrocarbons.
    • Aliphatic hydrocarbons, including saturated (alkanes), unsaturated (alkenes and alkynes)
    • Cyclic hydrocarbons, including alicyclic and aromatic hydrocarbons.

    Benzene Derivatives

    • Classification and naming conventions of benzene derivatives.
    • Examples of different benzene functional groups.

    Required Readings

    • Students are required to review a webpage on the history of medicinal chemistry.
    • A quiz is scheduled in the next session.

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    Introduction to Medicinal Chemistry PDF

    Description

    Explore the fascinating history and evolution of medicinal chemistry, beginning with ancient practices and transitioning through significant changes in the field. This quiz outlines the definitions of organic pharmaceutical chemistry and details the quantitative relationships crucial for understanding drug activity. Ideal for students interested in the intersection of chemistry and medicine.

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