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Med Chem Midterm > Lecture 1 Concept Notes > Flashcards

Lecture 1 Concept Notes Flashcards

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1
Q

SAR

A

Structure activity relationship:

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

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2
Q

MOA

A

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

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3
Q

ADME

A

Absorption, distribution, metabolism and excretion

can sometimes also include toxicity

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4
Q

Where is aspirin derived from?

A

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

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5
Q

Where is morphine derived from?

A

From opium poppy, a plant

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6
Q

How to define a good or a bad drug?

A

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

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7
Q

Medicinal Chemistry goal

A

improve drugs to the best of their ability

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8
Q

Therapeutic Index

A

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

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9
Q

T/F:
A small TI is good

A

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.

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10
Q

Warfarin, small therapeutic index. Explain

A

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.

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11
Q

Pencillin, large thereputic index

A

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

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12
Q

Name two ways a drug target can be validated

A

Gene Knockout, and RNAI (RNA interference )

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13
Q

Explain Gene Knockout

A

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

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14
Q

RNA interference

A

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

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15
Q

Receptors Validation

A

Validates the relationship between the receptor and the drug

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16
Q

Enzyme Validation

A

Validates how enzymes interact with the drug

17
Q

Ion channel validation

A

Validates how ion channels interact with the drug

18
Q

protein-protien interaction

A

interactions between proteins and the drug

19
Q

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

A

CoA receptors

20
Q

Natural Products

A

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

21
Q

Name three drugs that are natural products

A

Erythromycin A
Morphine
Lovastatin

22
Q

Natural product analogs
Semi-synthetic approach

A

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

23
Q

Examples of natural product analogs & what theyre synthesized from

A

Heroin and Oxycodone –> from Morphine

Simvastatin –> Lovastatin

Telitrhomycin –> Erythromycin

24
Q

Example of Natural product inspired agents

A

Methadone & Procaine

24
Q

Natural product inspired agents

A

Inspired from a natural product, but changes in significant ways

25
Q

Synthetic drugs (based on rational design)

A

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

26
Q

Example of a synthetic drug

A

Captopril

27
Q

Synthetic drug

A

Fully synthetically made

28
Q

HTS (high throughput screening)

A

Screens hundreds of thousands of compounds until a hit is found

29
Q

Examples of synthetic drugs

A

Clopidogrel (Plavix) or Imatinib (Gleevec)

30
Q

Serendipity in drug discovery

A

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

31
Q

Examples of serendipity

A

Penicillin or Viagra

32
Q

how was penicillin discovered

A

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

33
Q

what was viagra initially used for

A

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

34
Q
A

Med Chem Midterm (8 decks)

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