Drug design

Question 1

Three stages for drug design

Answer 1

Discovery
Optimization
Development

Question 2

Stage that involves drug target

Answer 2

Discovery

Question 3

Biochemical targets

Answer 3

Enzyme
GPCRs
Nuclear hormone receptors and transporters
Ion channels
Other receptors
DNA
Integrins

Question 4

Bioassays should be (3)

Answer 4

done in short period of time
handle a large number of samples
cost effective

Question 5

General types of Bioassays (using ——-)

Answer 5

whole organisms
mammalian cell cultures
purified enzymes or receptors
engineered microorganisms

Question 6

mechanism independent

Answer 6

non selective

Question 7

which are mechanism independent bioassays

Answer 7

whole organisms

mammalian cell cultures

Question 8

To process from crude mixture to pure compound what steps are needed (2)

Answer 8

Deconvolution

Dereplication

Question 9

Natural Products examples

Answer 9

Taxol
Erythromycin
Scopolamine
Tubocurarine

Question 10

Homologation

Answer 10

change the length of alkyl branch

-methyl, ethyl, propyl, butyl… chain reduction

Question 11

Chain branching

Answer 11

propyl, isopropyl

butyl, isobutyl

Question 12

Ring transformations

Answer 12

replace N-diethyl with pyrrolidine, piperidine, or piperazine rings

Question 13

Replace functional groups with bioisosteres

What are the examples for bioisosteres

Answer 13

Univalent atoms and groups
Bivalent atoms and groups
Trivalent atoms and groups
Tetravalent atoms and groups

Question 14

Lipinski’s Rule of five

Good molecules should have

Answer 14

molecular weight less than 500
fewer than 10 hydrogen bond acceptor
fewer than 5 H-bond donors
a C log P value of less than 5 ( a measure of water solubility)