Med Chem

Question 1

Wt’s rational inhibitor was for?

Answer 1

Laborious and resource-consuming screening processes - testing large numbers of synthetic chemicals or natural products for inhibitory against a chosen target enzyme.

Question 2

The effectiveness of an enzyme inhibitor will depend on

Answer 2

1. The potency of inhibitor
2. Its specificity toward its target enzyme.
3. The choice of metabolic pathway target for disruption.
4. Inhibitor or derivative possessing appropriate pharmacokinetic characteristics.

Question 3

Wt if drug very polar?

Answer 3

1. It can not cross cell menbrance

2. Transported by liposomes or nanoparticle

Question 4

In the Reversible En. Inhibitor What is Ki?

Answer 4

Is the association of the E-I complex.
Ki = [E][I]/[E-I]
The lower the better the inhibitor
DeltaG = RTlnKi
R is the universal gas constant
Small change in free energy will have significant effect on Ki

Question 5

Electrostatic force F =

Answer 5

q1q2/(r^2.D)
q1, q2 charged atoms
r is the distance between the charged groups
D dielectric constant of surrounding medium

Question 6

Ion-pair interaction is a long range interaction because

Answer 6

The strength of interaction decreases more slowly with distance

Dipoles interaction is a short range one.

Question 7

Why is the electrostatic interaction is less favorable in polar solvents?

Answer 7

because of its high net permanent dipole moment, water is very polar and has a large dielectric constant. The high polarity of H2O greatly diminishes the attraction or repulsion forces /./ any charged groups giving rise to the leveling effect of water.

Question 8

Other names of Van der Waals force?

Answer 8

nonpolar interaction

London dispersion forces