Lecture 1: Med Chem

Question 1

Drug

Answer 1

any substance that brings about a change in biologic function through its chemical actions

Question 2

biologics

Answer 2

protein drugs
increasing popularity

Question 3

Biological activity of a receptor requires a drug to:

Answer 3

1. move to receptor
2. bind to receptor

Question 4

Tubocurarine

Answer 4

muscle relaxant

Question 5

acetylcholine

Answer 5

neurotransmitter

same functional groups as tubocurarine but works opposite (quaternary amine)

Question 6

Pharmacophore

Answer 6

similar structural motif shared by drugs that bind to same target

responsible for BINDING to receptor

recognize active vs inactive compounds

3D structure matters

-other drug properties are affected by different parts of the drug this one is mostly for BINDING

Question 7

morphine

naloxone

fentanyl

Answer 7

-bind to opioid receptors
-contain piperidine ring and aromatic ring para to the nitrogen

Question 8

Morphine and Fentanyl

Answer 8

agonists

Question 9

naloxone

Answer 9

antagonist

Question 10

Structure-Activity Relationship

Answer 10

structure determines drug activity

modify structure = change properties

examine = predict

Question 11

Drug properties

Answer 11

dependent on chemical parts of molecule

binding strength, solubility, membrane crossing, degradation speed

Question 12

Structure

Answer 12

-Size
-Ionization
-Solubility
-Hydrophobicity
-Stereochemistry

Question 13

Activity

Answer 13

-membrane permeability
-target binding
-metabolism
-excretion

Question 14

Which of the following drug properties is determined by the STRUCTURE of the drug?

Answer 14

All of the above ?

Question 15

The structures of morphine and naloxone are shown below. Though their structures are quite similar, morphine is an agonist, and naloxone is an antagonist. What is the reasonable explanation of this difference in drug activity?

Answer 15

Morphine activates the receptor, but naloxone does not.

Question 16

What does SAR stand for?

Answer 16

structure-activity relationship

Question 17

The structure of tubocurarine is shown below. Tubocurarine had been used by the South American natives as arrow poison, but they did not experience any adverse effect when they consumed the contaminated meat. What is the reasonable explanation for this?

Answer 17

The poison is not active orally because it has a quaternary amine group.

Question 18

Based on the drug activities and the simplified structures of the four following analogous drugs, which of the following statement is INCORRECT?

A. The drugs need the half circle for binding to the receptor.
B. The drugs need the half circle for proper solubility.
C. The common half circle region of the active drugs is called a pharmacophore.
D. When the structure of the half circle region is altered, the active drugs may lose their activities.

Answer 18

-drugs need the half-circle for solubility