1) The following compounds all belong to the same broad class of antibacterial drugs. Rank them in order
from most potent (1) to least potent (3) based on their intrinsic activity at enzyme inhibition (e.g., an in
vitro assay). Explaining your reasoning is an important part of getting full credit.
2) A patient with a bacterial infection was treated with penicillin derivative D, (shown below) but the
infection persisted. When treated with a combination of D and E, the infection was cured, although E by
itself was inactive. Can you explain why this occurred and suggest a single penicillin drug that would be
effective for treating this specific infection?
3) Compound F is a potent and non-selective -agonist called isoproterenol. A similar compound with a
single meta-hydroxy group and replacement of the N-isopropyl with a methyl group gives a drug (G) with
only 1 agonist activity and no activity. If the pattern of hydroxy groups is switched from 1,2 in
isoproterenol to 1,3, compound H is prepared. H has selective 2 agonist activity and when dosed in
humans, has a much longer duration of action. Please be very specific in your answers to the following
a) What are two reasons why G does not have activity?
b) Why does adding another meta-hydroxy group (H) return activity?
c) Why does H have a longer duration of action?
4) Describe each of the follow compounds as having the potential to act as either; 1) non-selective antagonist, 2) short acting -antagonist, 3) 2-agonist or 4) long acting -antagonist. Do not waste
time looking these compounds up (I made them up), I want you to use your knowledge of the subject to
make the determination.
5) The compound shown below has almost no activity when tested in an in vitro assay. When dosed in
humans, many find it to be an excellent pain reliever while others find it to be ineffective. Whats going, be
very specific with your explanation including any analogous compounds you may wish to compare this
6) Congratulations on your fine work as a medicinal chemist at the ACME Pharmaceutical Company! Your
work in the hypotension group (lowering blood pressure) has come up with a great new drug candidate
While this compound was efficacious in lowering blood pressure in clinical trials, it was seen that in
patients that had infections and were treated with sulfmethoxazole, the infection persisted. On the other
hand, those infected patients treated with penicillins were cured from the infection. Please explain.
7) Based on your knowledge of the different classes of drugs we have studied in the second half of this
class, please answer the following questions based on the structure shown below. This drug has very little
metabolism and is excreted mostly as the molecule shown.
a) What class or type of drugs would you most associate this drug with? What features lead you to this
b) What part of the body would this drug not be effective in? Why?
c) What clinical indication might this drug be prescribed for? Why?
8) Your success at ACME is known throughout the company and your supervisor places you on a lead
discovery program. The aim of this project is to identify a potent (IC 50 << 1 M) and reversible inhibitor of
a particular enzyme. You have a discussion with your friendly biochemist also on the project and together
you decide to set up a screen to look for fragments. The project churns along and after screening ACMEs
fragment file, the following compounds and their corresponding activities are identified:
All of these compounds are believed to bind in the active site of the enzyme. Be specific in explaining a
strategy to move forward including a compound to prepare (you dont need to synthesize it).
9) Youve been so successful at ACME that you have been moved to the antibacterial program with the
hope that you can provide a winner there as well. In your first project looking at an SAR program around
the cephalosporin Cefuroxime, you prepare the compound shown below.
Your biologist calls you screaming with great news, in the in vitro assay, this compound is over 100 times
more active than the Cefuroxime standard. Of course you reply, I planned this happen. Please explain
this to your biologist.
10) Please rank the following drugs for their analgesic activity when dosed in an IV formulation. 1=most
active and 4=least active. Explain your reasoning.
The post Question1) The following compounds all belong to the same broad class of antibacterial drug appeared first on WriteDen.
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