Structure-Activity Relationships (SARs) in Medicinal Chemistry for MPharm Students

Question 1

Which factor does NOT influence the structure-activity relationship (SAR) of a drug?

Accepted Answer

Pharmacokinetics

Answer

Molecular shape

Answer

Electronic properties

Answer

Binding affinity

Question 2

A drug with stronger binding affinity to its target is likely to have:

Accepted Answer

Increased potency

Answer

Decreased efficacy

Answer

Reduced bioavailability

Answer

Increased toxicity

Question 3

The concept of bioisosteres involves:

Accepted Answer

Molecules with similar electronic properties but different structures

Answer

Molecules with identical structures but different electronic properties

Answer

Molecules with similar structures and different electronic properties

Answer

Molecules with different structures and different electronic properties

Question 4

Which of the following is NOT a factor that can influence the structure-activity relationship (SAR) of a drug?

Accepted Answer

Patient age

Answer

Molecular weight and shape

Answer

Electronic properties

Answer

Solubility

Question 5

The process of designing a drug's structure to optimize its activity and minimize its side effects is known as:

Accepted Answer

Rational drug design

Answer

Molecular docking

Answer

High-throughput screening

Answer

Pharmacophore modeling

Question 6

Which of the following functional groups typically increases a drug's solubility?

Accepted Answer

Alcohol

Answer

Aromatic ring

Answer

Carboxylic acid

Answer

Ketone

Question 7

A drug that binds to a receptor and triggers a biological response is known as an:

Accepted Answer

Agonist

Answer

Antagonist

Answer

Inverse agonist

Answer

Partial agonist

Question 8

The quantitative measure of a drug's affinity for its target is termed:

Accepted Answer

Potency

Answer

Efficacy

Answer

Selectivity

Answer

Solubility

Question 9

Which of the following is an example of a prodrug?

Accepted Answer

Enalapril

Answer

Aspirin

Answer

Ibuprofen

Answer

Acetaminophen

Question 10

The lipophilicity of a drug is a measure of its:

Accepted Answer

Affinity for lipids

Answer

Solubility in water

Answer

Size and shape

Answer

Biological activity

Question 11

Which of the following factors is not typically considered in quantitative structure-activity relationship (QSAR) studies?

Accepted Answer

Patient demographics

Answer

Molecular structure

Answer

Biological activity

Answer

Physicochemical properties

Question 12

In the context of SARs, the term 'pharmacophore' is used to describe what?

Accepted Answer

The three-dimensional arrangement of molecular features essential for drug activity.

Answer

The specific protein target that a drug binds to.

Answer

The chemical scaffold that forms the backbone of a drug molecule.

Answer

The metabolic pathway involved in drug elimination.

Question 13

Consider the following series of compounds: Compound A has a partition coefficient (logP) of 2, while Compound B has a logP of 4. Which compound is more likely to exhibit good oral bioavailability?

Accepted Answer

Compound B

Answer

Compound A

Answer

Both compounds have equal chances of good oral bioavailability.

Answer

Neither compound is likely to exhibit good oral bioavailability.

Question 14

Which of the following factors does **not** influence the structure-activity relationship of a drug molecule?

Accepted Answer

Patient's **age** and **gender**

Answer

Molecular size and shape

Answer

Chemical structure and functional groups

Answer

Biological target

Question 15

The lipophilicity of a drug molecule is measured by its:

Accepted Answer

Partition coefficient

Answer

Polar surface area

Answer

Molecular weight

Answer

Number of hydrogen bond donors

Question 16

Which of the following interactions is **not** considered a non-covalent interaction in drug-target binding?

Accepted Answer

Covalent bonding

Answer

Hydrogen bonding

Answer

Ionic bonding

Answer

van der Waals forces

Question 17

The quantitative measure of the affinity between a drug and its target is:

Accepted Answer

Equilibrium dissociation constant (Kd)

Answer

Potency

Answer

Efficacy

Answer

Solubility

Question 18

The study of the relationship between the structure of a drug and its toxicity is known as:

Accepted Answer

SAR toxicology

Answer

Toxicology

Answer

Toxicokinetics

Answer

Toxicodynamics

Question 19

Which of the following is a lipophilicity parameter commonly utilized in SARs?

Accepted Answer

LogP

Answer

EC₅₀

Answer

pKa

Answer

IC₅₀

Question 20

Which approach is commonly adopted to enhance drug potency?

Accepted Answer

Introducing bulky substituents to the molecule

Answer

Reducing the number of aromatic rings

Answer

Increasing the polarity of the molecule

Answer

Decreasing the molecular weight

Question 21

Which of the following is NOT a factor that can influence the structure-activity relationship (SAR) of a drug molecule?

Accepted Answer

Molecular weight

Answer

Lipophilicity

Answer

Electronic properties

Question 22

The Hansch equation is primarily used to quantify the relationship between:

Accepted Answer

Structure and biological activity of drug molecules

Answer

Molecular weight and toxicity of compounds

Answer

Polarity and solubility of molecules

Answer

Lipophilicity and potency of molecules

Question 23

Which of the following is a widely used approach for studying structure-activity relationships (SARs)?

Accepted Answer

Quantitative structure-activity relationship (QSAR) modeling

Answer

In vitro cell culture assays alone

Answer

Animal models exclusively

Question 24

The concept of a pharmacophore refers to:

Accepted Answer

The essential structural features required for biological activity of a drug molecule

Answer

The specific binding site of a receptor

Answer

The three-dimensional structure of a drug molecule

Question 25

Which technique is primarily used to identify the binding site of a drug on a target protein?

Accepted Answer

Molecular docking

Answer

Nuclear magnetic resonance (NMR) spectroscopy

Answer

X-ray crystallography

Answer

Mass spectrometry

Question 26

Lipophilicity is an essential property of drug molecules because it influences their:

Accepted Answer

Ability to cross biological membranes

Answer

Rate of metabolism

Answer

Solubility in water

Answer

Rate of excretion from the body

Question 27

Which of the following is a common type of noncovalent interaction involved in drug-target binding?

Accepted Answer

Hydrogen bonding

Answer

Ionic bonding

Answer

Van der Waals forces

Answer

Covalent bonding

Question 28

The concept of prodrugs is primarily used to:

Accepted Answer

Enhance drug delivery and efficacy

Answer

Improve drug solubility solely

Answer

Increase drug absorption exclusively

Answer

Reduce drug toxicity primarily

Question 29

Which of the following is a crucial step in the process of drug development aimed at improving a lead compound?

Accepted Answer

Structure-activity relationship (SAR) studies

Answer

Clinical trials alone

Answer

Phase I trials exclusively

Answer

Preclinical testing solely