Name______________________________________CHEM 4170 Exam 1 all answers must fit in sp ace provid ed
1
Matching (22 pts). Place the Letter of the Best
Answer in the Blank on the Left
1. Pharmacokinetics __N___
2. Pharmacodynamics __J___
3. Pharmacophore __L___
4. Autocoid ___C___
5. X-ray crystallography __F___
6. Covalent Bond ___H__
7. van der Waals interaction __D___
8. Hydrogen Bond __R___
9. Ionic Bond __G___
10. QSAR __P___
11. KB __A___
A. = 1/KD
B. Any compound used to cure, mitigate, prevent, or diagnose
a disease or physical malady
C. Endogenous ligand for a receptor
D. Strength varies as 1/r6 (r = distance)
E. = [D][R]/[D•R]
F. Can provide a three-dimensional picture of a
macromolecular drug target
G. Strength varies as 1/r2 (r = distance)
H. Stable bond at room temp. Worth 85 kcal/mol
I. Stable bond at room temp. Worth 8.5 kcal/mol
J. Interaction of drug with its biological target
K. Quantitative system to assay receptors
L. Core set of functional groups required for biological
activity within a structural group of molecules
M. Often thermoneutral a vaccum
N. Absorbtion, distribution, metabolism, excretion, and
toxicity
O. Favored by electron withdrawing groups
P. Quantitative structure-activity relationship
Q. Qualitative stereochemistry assessment ratio
R. Strongest when bond angle is 180˚
12. (5 pts). Why were almost all early, successful medicines derived from plants?
Answer: See class notes regarding the early history of medicinal chemistry
13. (6 pts). List one advantage and two disadvantages of an in vivo bioassay for lead discovery.
i. Answer: See class notes regarding bioassays.
ii.
iii.
14. (5 pts). Addition of an ionic interaction worth –6.8 kcal/mol will alter the binding constant of a
drug by a factor of about (circle the best answer and briefly show how you calculated your answer):
Answer: 100,000. Must show equation that you used to calculate. See handout on Keq/G
0.01 0.1 3.4 10 100 1000 10,000 100,000 1,000,000
