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Principles of Bioorganic Medicinal Chemistry Drugs & Medicinal Chemist . Lovastatin-Mevacor. August 26/2002. Zbigniew J. Witczak, Ph.D. Principles of Bioorganic & Medicinal Chemistry PHA 598A: Dr. Zbigniew J. Witczak. Learning Objectives

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Principles of Bioorganic Medicinal Chemistry

Drugs & Medicinal Chemist

Lovastatin-Mevacor

August 26/2002.

Zbigniew J. Witczak, Ph.D.


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Principles of Bioorganic & Medicinal Chemistry PHA 598A: Dr. Zbigniew J. Witczak

Learning Objectives

1. Describe the mechanism by which cell macromolecules mediates the cellular response.

2. Identify the cell components and active macromolecules that are involved in the development and regulation of the cellular processes and drug action/response.

3. Identify the pharmacological responses by which the therapeutic agents acts in the multiple cellular system.

4. Identify the chemical aspects of drug action and their pharmacological responses.


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Clasification of Drugs

  • by pharmacological effect

  • by chemical structure

  • by target system

  • by site of action


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By pharmacological effect

  • analgesics

  • antipsychotics

  • antihypertensive

  • antiasmathics

  • antibiotics

  • anticonvulsant (sedative agents)


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By chemical structure

  • Opiates

  • Steroids

  • Barbiturates

  • Penicilins

  • Cateholamines

Penicillin V


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  • Why should drugs work?

    • Cell/cell membranes

  • Where do drugs work?

    • Cell/cell membranes

    • Nucleus- “control centre” for the cell


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    Molecular Targets in the Cell Affected by Drugs

    • Lipids

    • Proteins (Glycoproteins)

    • Nucleic acids


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    Fatty acids and other lipids.


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    Fatty acids and other lipids.


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    Therapeutic Index ******

    • Measure of the ratio of undesirable to desirable drug effects.

    • For in vivo systems thee therapeutics index could be the ratio of the LD50

      ( the lethal dose for 50 % of the test animals) to the ED50 ( the effective

      dose that produces the maximum therapeutic effect in 50 % of the test animals.

    • The larger the therapeutic index the greater the margin of safety of the drug!!!!.


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    Hydrophilic

    Hydrophilic

    Hydrophilic

    Hydrophobic Region

    Amphotericin B

    • Amphotericin B interacts with the lipids of fungal cell membranes

    • Build “Tunnels” through the membrane

    • The contents of the cell is drained away

    • Cell is killed


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    Inhibitors of Glycosphingolipid Biosynthesis


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