MCMP 824: Lecture 6

Question 1

we use this as a way we can take the potency of a series of drug molecules and then assess their efficacy in a quantitative fashion with respect to a variety of parameters such as lipophilicity, electronic steric factors, etc.

Answer 1

QSARs

Question 2

QSAR should give us what type of graph

Answer 2

parabolic

Question 3

an _________ is a compound that resembles an essential metabolite and _____ with the metabolite in physiological reactions

Answer 3

• antimetabolite

- competes

Question 4

a lot of drugs are _____ _____. To make inhibitor is to design it based on ____ of its natural state.

Answer 4

• enzyme inhibitors

- analogs

Question 5

common drug strategy is to go after ____ that are essential for?

Answer 5

• metabolites

- life and growth

Question 6

bioisosteres are functional groups or atoms that have 1 + 2 + 3

Answer 6

1) similar steric and electronic properties
2) produce similar effects on target
3) but have improved pharmacokinetics

Question 7

knowledge of bioisosteres is coupled with the ability to identify a _____ (if we found a pair of bioisosteres, then we can more easily recognize the pharmacophore, or if we know the pharmacophore, we can more easily find bioisosteres

Answer 7

• pharmacophore

Question 8

drug design is a real multiobjective optimization problem. Not just designing for ____ to ____ ____. We have to design for _____, _____, etc.

Answer 8

• binding, protein target

- absorption, distribution

Question 9

a ______ is an inactive or “carrier” form of a drug that is transformed inside the body, usually _____ to the active form of the drug

Answer 9

• prodrug

- enzymatically

Question 10

a prodrug can (5)

Answer 10

1) prolong or shorten the duration of action
2) help localize a drug to a specific target site
3) take advantage of active transport processes
4) solve a formulation problem
5) decrease toxicity or side effects