Lecture 1 Concept Notes

Question 1

SAR

Answer 1

Structure activity relationship:

How the structure of the drug affects how the drug functions in the body

Question 2

MOA

Answer 2

Mechanism of Action
How the drug reacts with targets in the body on a molecular level

Question 3

ADME

Answer 3

Absorption, distribution, metabolism and excretion

can sometimes also include toxicity

Question 4

Where is aspirin derived from?

Answer 4

Willow tree bark contains salicylic acid which is one of the precursors for aspirin

Question 5

Where is morphine derived from?

Answer 5

From opium poppy, a plant

Question 6

How to define a good or a bad drug?

Answer 6

Subjective. Can depend on how the drug interacts and side effects in the body. Too much of any drug can be harmful

Question 7

Medicinal Chemistry goal

Answer 7

improve drugs to the best of their ability

Question 8

Therapeutic Index

Answer 8

The ratio between the therapeutic effect & the toxicity of the drug.

Question 9

T/F:
A small TI is good

Answer 9

False.

We want the therapeutic index to be as large as possible. This means we can give multiple or higher doses of a drug before the drug starts to have toxic effects on the body.

Question 10

Warfarin, small therapeutic index. Explain

Answer 10

If another dose is given of warfarin, it increases the chance of the drug causing issues in the body. There is unwanted adverse effects with a smaller dose of warfarin.

Question 11

Pencillin, large thereputic index

Answer 11

Multiple doses or higher doses of penicillin are okay, and will not cause unwanted adverse effects in the body

Question 12

Name two ways a drug target can be validated

Answer 12

Gene Knockout, and RNAI (RNA interference )

Question 13

Explain Gene Knockout

Answer 13

When a gene is removed from expressing to see how a disease progresses without it.

Question 14

RNA interference

Answer 14

reduces expression through RNA molecules and gives insights as to how disease progression occurs without that gene

Question 15

Receptors Validation

Answer 15

Validates the relationship between the receptor and the drug

Question 16

Enzyme Validation

Answer 16

Validates how enzymes interact with the drug

Question 17

Ion channel validation

Answer 17

Validates how ion channels interact with the drug

Question 18

protein-protien interaction

Answer 18

interactions between proteins and the drug

Question 19

Example of a biological target: Lipitor (dont need to know but to explain the concept)

Answer 19

CoA receptors

Question 20

Natural Products

Answer 20

fully derived from a natural product like a fungi, bacteria, plants, etc.

Question 21

Name three drugs that are natural products

Answer 21

Erythromycin A
Morphine
Lovastatin

Question 22

Natural product analogs
Semi-synthetic approach

Answer 22

Drug is edited from a natural product and some functional groups change

Question 23

Examples of natural product analogs & what theyre synthesized from

Answer 23

Heroin and Oxycodone –> from Morphine

Simvastatin –> Lovastatin

Telitrhomycin –> Erythromycin

Question 24

Example of Natural product inspired agents

Answer 24

Methadone & Procaine

Question 24

Natural product inspired agents

Answer 24

Inspired from a natural product, but changes in significant ways

Question 25

Synthetic drugs (based on rational design)

Answer 25

Created rationally
Ex- finding a substrate that fits into an enzyme and creating a drug that looks like the substrate that wont be metabolized, but rather prevent the enzyme from working

Question 26

Example of a synthetic drug

Answer 26

Captopril

Question 27

Synthetic drug

Answer 27

Fully synthetically made

Question 28

HTS (high throughput screening)

Answer 28

Screens hundreds of thousands of compounds until a hit is found

Question 29

Examples of synthetic drugs

Answer 29

Clopidogrel (Plavix) or Imatinib (Gleevec)

Question 30

Serendipity in drug discovery

Answer 30

Drugs that are discovered by accident, or for another indication.

Question 31

Examples of serendipity

Answer 31

Penicillin or Viagra

Question 32

how was penicillin discovered

Answer 32

It was observed that penicillin inhibits bacterial growth on a mold plate

Question 33

what was viagra initially used for

Answer 33

Viagra was initially use for chest pains and found to be useful for erectile dysfunction