Exam 2

Question 1

What is hybridization for tetrahedral geometry?

Answer 1

sp3

Question 2

What is hybridization for octahedral geometry?

Answer 2

sp3d2

Question 3

What is hybridization for square planar geometry?

Answer 3

sp3d2

Question 4

Define a metal ion complex

Answer 4

A complex with a metal ion bonded to a number of ligands.

Question 5

What is a Lewis acid?

Answer 5

An acceptor, typically a metal ion.

Question 6

What is a Lewis base?

Answer 6

A donor, typically ligands.

Question 7

What is the chelate effect?

Answer 7

More stable complexes are formed with chelating agents than with the equivalent number of monodentate ligands.

Question 8

What is EDTA4-?

Answer 8

A chelating agent that occupies 6 coordination sites.

Question 9

What is the probable mechanism for charge transfer in organic molecular complexes?

Answer 9

Charge transfer from nonbonded electrons on N or S to iodine.

Question 10

Name a drug used to treat alcohol addiction.

Answer 10

Disulfiram

Question 11

What type of activity does cholomethiazole have?

Answer 11

Sedative-hypnotic

Question 12

What is the function of tolnaftate?

Answer 12

Antifungal

Question 13

What is the significance of cis and trans in molecular geometry?

Answer 13

Cis means same side of the plane, trans means opposite side of the plane.

Question 14

Which has greater muscarinic activity: erythro or threo?

Answer 14

Erythro

Question 15

What is a rigid analog in drug design?

Answer 15

A conformationally rigid compound synthesized to overcome obstacles.

Question 16

Define an agonist in pharmacology.

Answer 16

A compound that has affinity for the receptor and intrinsic activity.

Question 17

Define an antagonist in pharmacology.

Answer 17

A compound that has affinity but lacks intrinsic activity.

Question 18

True or False: Most drug-receptor interactions are non-covalent and reversible.

Answer 18

True

Question 19

What are covalent bonds?

Answer 19

The strongest bonds formed by sharing electron pairs, generally irreversible.

Question 20

What is the role of hydrogen bonds in drug interactions?

Answer 20

Formed by hydrogen atoms bonded to F, O, or N.

Question 21

What type of bond occurs between ions of opposite charge?

Answer 21

Ionic bonds

Question 22

What are hydrophobic bonds?

Answer 22

Interactions between alkyl and aryl groups in water.

Question 23

What characterizes an active/unconfirmed hit?

Answer 23

It demonstrates some predetermined level of activity.

Question 24

What is a confirmed hit?

Answer 24

A compound that has gone through hit validation to ensure activity isn’t due to artifacts.

Question 25

What is lead optimization?

Answer 25

The process that begins with a compound displaying interesting biological action and ends with identifying the best analog.

Question 26

What are drugs?

Answer 26

Molecules that affect biological processes and are used to treat disease.

Question 27

What is required for a drug's safety?

Answer 27

It must have a specific action.

Question 28

How long does the discovery of a new chemical entity typically take?

Answer 28

12-20 years.

Question 29

Why are esters and amides less activating than esters and amines?

Answer 29

Lone pairs on O in esters and amides participate in resonance with the C=O group.

Question 30

Why are amines better activators than alcohols?

Answer 30

Nitrogen is less electronegative than oxygen.

Question 31

What is Lipinski's Rule of 5?

Answer 31

Guidelines for orally active compounds.

Question 32

What is a rich source of biologically active compounds in drug discovery?

Answer 32

The plant kingdom.

Question 33

What are secondary metabolites?

Answer 33

Compounds that can act as lead compounds in drug discovery.

Question 34

What is a common source of lead compounds in drug discovery?

Answer 34

Microorganisms.

Question 35

What is a notable source of lead compounds from marine sources?

Answer 35

Coral and sponges.

Question 36

What is the significance of venom and toxins in drug discovery?

Answer 36

They are extremely potent and have very specific interactions with macromolecular targets.

Question 37

What is combinatorial synthesis?

Answer 37

Automated solid-phase procedure aimed at producing many different structures in a short time.

Question 38

What is parallel synthesis?

Answer 38

Small scale synthesis of a large number of compounds, each reaction vial contains a distinct product.

Question 39

What does the rule of 3 in fragment-based lead discovery entail?

Answer 39

Molecule less than 300, no more than 3 hydrogen bond donors, clogP=3, no more than 3 rotational bonds.

Question 40

What is the purpose of drug biotransformation?

Answer 40

To detoxify and increase elimination.

Question 41

What is Phase 1 in biotransformation?

Answer 41

Introducing polar functionality to a molecule.

Question 42

What is Phase 2 in biotransformation?

Answer 42

Attaching small polar groups to the molecule.

Question 43

What is the importance of 3D molecular geometries?

Answer 43

They influence biological, physical, and chemical properties.

Question 44

What is a lead compound in medicinal chemistry?

Answer 44

A compound that acts as the starting point for drug design and development.

Question 45

What is the most commonly used drug with an ester?

Answer 45

Aspirin.

Question 46

Which functional group is likely to participate in dipole-dipole interactions?

Answer 46

Ketone.

Question 47

What are the relative strengths of different types of bonds from strongest to weakest?

Answer 47

Covalent > Ionic > H-bond > Van der Waals.