Medicinal Chemistry – Exam 1


A Drug is any chemical that can react with biological systems and produce a biological response.

(Cocaine, Caffeine, Aspirin, even Water)

Why Does A Drug Work?

-All life is made up of cells

-All cells are made up of chemical components

-Cells are chemical factories, with innumerable chemical reactions taking place

-When a new chemical is introduced to a cellular system, it will have an effect!

CHALLENGE – Having the Desired Effect


Good Drug – Cures diseases

Bad Drug – Causes unwanted effects


All drugs have unwanted side effects, no such thing as a perfect drug

ZERO drugs without unwanted side effects



Pharmological Effect

Drugs are classified by their desired outcome and effect

-Many drugs have more uses than one (many different purposes)

Classification Examples – analgesics, antipsychotics, antibacterials, antibiotics

Drug Classification

Chemical Structure

Structures to Know: Penicillins, Opiates, Barbiturates, Steroids

Compounds with a common skeleton

Why is this useful? – compounds of similar structures have similar activities (SAR)

**Different Structures have different biological actions**




Medicinal Chemistry

Science that deals with the discovery and design of new chemicals and their development into useful medicines



Various Fields of Study in Medicinal Chemistry

-Computational Chemistry

-Synthesis of New Compounds

-SAR Investigation

-Understanding Interactions of chemical w/ receptors like DNA, enzymes, etc.

-Absorption, transport, distribution properties

-Metabolism or Breakdown




Benefits of Modern Drug Development

-Life threatening diseases have become minor health problems (polio, small pox, TB, gastric ulcers)

-Life Expectancy has increased

-Improvement in Quality of Life




Consequences of Drug Development

-Overuse of Antibiotics -> Bacterial Resistance

-A more healthy elderly population, leading to more diseases of the elderly

Ex/ Cancer, autoimmune diseases, neurodegenerative diseases (Alsheimers), and degenerative diseases






usually located in the cell membrane; trigger responses on the outside of the cell and relay signals to the inside of the cell. Receptors are also capable of linking to enzymes, causing a chemically reactive response






A protein that can be bound to a membrane or free floating within a cell; facilitate chemical change when bound to a substrate; catylyst






Has affinity for a receptor and produces a bioresponse






Has an affinity to a receptor and doesn’t produce a bioresponse, meaning it has no intrinsic activity





Choose A Disease!

-Needs to be one that needs new and improved drugs

-Marketing decision; most market to a first world disease such as migraines, cardiovascular diseases, ulcers, cancer, flu, depression, or obesity

-Third World diseases bring life expectancy to 40 years of age and below are usually ignored, however treatments for malaryia are now being developed for treatment and evaluated




Choose a Drug Target!

-The reference sequence for the human genome has been revealed and therefore there are more options for targets than compounds to interact with them.

-Now trial and miss with selected targets while utilizing the components of a known drug, or a known drug in it’s entirety, instead of developing new drugs and trial and missing aimlessly

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