Lecture 2 done

Question 1

What is lipinski’s rule of 5?

Answer 1

Poor absorption or permeation is more likely when there are more than 5-H bond donars, 10 H-bond acceptors, molecular weight> 500 and calculated Log P is greater than 5

Question 2

What is Veber’s rule for drug like molecules?

Answer 2

1)10 or fewer rotatable bonds
2)polar surface area equal to or less than 140 A

Question 3

What properties are assesed for drug likeness?

Answer 3

molecular weight, HB acceptors and donors, polar groups, rotatable bonds, chirality, Log P (oil/water partition coefficient)

Question 4

What do you need to predict the rate of drug action?

Answer 4

aqueous solubility, dissolution rate, acid/base ionization constant, pereability, stability

Question 5

True or False: Most drugs are large molecules (greater than 400 g/mol)

Answer 5

False. Most are small molecules less than 400 g/mol. This is one of Lipinski’s rules

Question 6

What are common h-Bond donars?

Answer 6

-OH, NH

Question 7

What are common H-bond acceptors?

Answer 7

-O, -N

Question 8

What is considered a rotatable bond?

Answer 8

a carbon single bond attached to anothe non hydrogen atom
(except for N)

Question 9

What is a chiral molecule?

Answer 9

mirror image is different from each other

Question 10

Can chirality impact efficacy and toxicity?

Answer 10

yes. some isomer changes can cause birth defects

Question 11

Out of a survey of 1000 drugs, what is the most common number of H_bond donars?

Answer 11

3

Question 12

Out of a survey of 1000 drugs, what is the most probable number of H-bond acceptors?

Answer 12

5

Question 13

Why is H-bonding important for a drug?

Answer 13

many drug-protein binding interactions occur through HBs

Question 14

How many rotatable bonds do drugs have on average?

Answer 14

5-10

Question 15

True or False: Synthetic drugs are equally flexible in comparison to natural drugs.

Answer 15

False. Synthetic drugs are a little more flexible.