Medicinal Chemistry and Drug Design Flashcards
6 cards from real MPharm Master of Pharmacy practice questions. Tap to flip, then mark Knew It or Still Learning — missed cards come back until you master them.
Read the first 6 Medicinal Chemistry and Drug Design flashcards as text
What is the primary purpose of the Lipinski Rule of Five in drug design?
Answer: Predict oral bioavailability based on physicochemical properties
Lipinski's Rule of Five predicts whether a drug candidate has physicochemical properties likely to result in good oral absorption and bioavailability.
Which functional group is most commonly targeted by irreversible inhibitors to form a covalent bond with an enzyme?
Answer: Serine hydroxyl group
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.
In structure-activity relationship (SAR) studies, what does the bioisostere concept involve?
Answer: Substituting a group with another of similar size and electronics to maintain activity
Bioisosteric replacement substitutes one atom or group with another having similar steric and electronic properties to retain or improve biological activity.
What is the pharmacophore of a drug?
Answer: The minimum structural features required for biological activity
A pharmacophore defines the essential 3D arrangement of atoms and functional groups needed for a drug to interact with its target and produce activity.
Which technique is used in fragment-based drug discovery (FBDD) to detect weak fragment binding to a target protein?
Answer: Surface Plasmon Resonance (SPR)
SPR measures real-time binding events between a fragment and an immobilized target protein by detecting changes in refractive index.
Prodrugs are designed primarily to address which drug property limitation?
Answer: Poor absorption or membrane permeability
Prodrugs are inactive precursors converted in vivo to the active drug, improving absorption, permeability, or stability of the parent compound.