MPharm Master of Pharmacy Medicinal Chemistry and Drug Design 1

Question 1

What is the primary purpose of the Lipinski Rule of Five in drug design?

Accepted Answer

Predict oral bioavailability based on physicochemical properties

Answer

Lipinski's Rule of Five predicts whether a drug candidate has physicochemical properties likely to result in good oral absorption and bioavailability.

Question 2

Which functional group is most commonly targeted by irreversible inhibitors to form a covalent bond with an enzyme?

Accepted Answer

Serine hydroxyl group

Answer

Many irreversible inhibitors react with the serine hydroxyl in the enzyme's active site, as seen with aspirin's acetylation of COX-1 serine residue.

Question 3

In structure-activity relationship (SAR) studies, what does the bioisostere concept involve?

Accepted Answer

Substituting a group with another of similar size and electronics to maintain activity

Answer

Bioisosteric replacement substitutes one atom or group with another having similar steric and electronic properties to retain or improve biological activity.

Question 4

What is the pharmacophore of a drug?

Accepted Answer

The minimum structural features required for biological activity

Answer

A pharmacophore defines the essential 3D arrangement of atoms and functional groups needed for a drug to interact with its target and produce activity.

Question 5

Which technique is used in fragment-based drug discovery (FBDD) to detect weak fragment binding to a target protein?

Accepted Answer

Surface Plasmon Resonance (SPR)

Answer

SPR measures real-time binding events between a fragment and an immobilized target protein by detecting changes in refractive index.

MPharm Master of Pharmacy Practice Test

MPharm Master of Pharmacy Practice Test

MPharm Master of Pharmacy Medicinal Chemistry and Drug Design 1