Principles of Medicinal Chemistry Review of Organic Functional Groups II. September 16/2002. Zbigniew J. Witczak, Ph.D. Principles of Medicinal Chemistry PHA 421: Dr. Zbigniew J. Witczak. Learning Objectives After completion of theses lectures students should be able to:
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Principles of Medicinal Chemistry
Review of Organic Functional Groups II
Zbigniew J. Witczak, Ph.D.
After completion of theses lectures students should be able to:
Important Functional Groups on Drugs II
Metabolic Reactions of the Phenol Functional Groups
Metabolic dealkylation of anisole
Aldehydes and Ketones
Minor oxidation of aldehydes
Which group on the compound is most & least acidic.
Functional derivatives of Carboxylic Acids
Structure –Activity Relationships in Drug Action
R = H, Noradrenaline
R = Me Adrenaline
g-aminobutiric acid (GABA)
Structures of Clinically Useful Sulfonamides
R = pKa = 6.9
R = pKa = 5.45
Schematic Actions of Sulfonamides and Trimethoprim
How prodrugs are made
Chemical Delivery Systems: Pharmacologically inactive molecules that require several steps of chemical and/or enzymatic conversion to the active drug and enhance drug delivery to particular organs or sites. Example: Brain-specific chemical delivery system
Soft Drugs: Biologically active, therapeutically useful chemical molecules (drugs) characterized by a predictable and controllable in vivo deactivation, after achieving the therapeutic objective, to nontoxic, inactive compounds
2. Improving drug delivery
The pro-drug by its improved characteristics gets closer to the receptor site for a longer period of time, and conversion to the parent drug takes place at the site of action.