Chem Basis CPN structures 3

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kyleannkelsey
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258476
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Chem Basis CPN structures 3
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2014-01-28 16:31:18
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Chem Basis CPN structures
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Chem Basis CPN structures 3
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  1. What CPNs have are cephamycins?
    Cefoxitin and Cefotetan

  2. Creating a prodrug from COOH has what effect on a CPN?
    Enhance absorption rate, minimized acid catalyzed degradation, twice daily dosing
  3. Do CPNs penetrate the CNS well?
    No, some in 2nd and 3rd gen do though
  4. Can a 3rd generation CPN that penetrates the BBB, be sued to treat a Staphylococcal meningitis infection?
    No, 3rd gen CPNs have poor G+ coverage
  5. Why do 3rd gen CPNs have some BB penetration capabilities?
    Have enough polarity

  6. Compare the G+ coverage of these two drugs:
    Cefepime has greater G+ coverage because it is less polar, see the R’ substituents

  7.  Is cefepime a good choice for treatment of a bacterial infection that is resistant to Ceftazidime and other 3rd gen CPNs?
    Yes

  8. How do these two drugs compare in B-lactamase resistance?
    Cefepime has greater B-lactamase resistance

  9. (True/False) An ester for the carboxylic group produces an active drug with enhanced absorption.
    False, it would not be active

  10. (True/False) methoxy at -C7 produces cephamycin series with enhanced beta-lactamase resistance.
    True

  11. What is this drug?
    Ceftaroline

  12. Ceftaroline is known for what special spectrum enhancements?
    Expanded G+ coverage to include Staph aureus and streptococcus pneumoniae

  13. Does Cefaroline’s spectrum cover P. auruginosa?
    No

  14. Does Ceftaroline have a larger G- spectrum than other CPNs?
    No, similar G- coverage

  15. The Ceftaroline phosphono group has what characteristics?
    Increases solubility (not present in activated drug)

  16. The Ceftaroline 1,2,4 thiadiazole ring has what characteristics?
    Good G- penetration and transpeptidase activity due to its polarity

  17. The Ceftaroline Oxime group has what characteristics?
    Enhances B-lactamase resistance

  18. The 1,3 thiazole ring on Ceftaroline hs what characterisitcs?
    Anti-MRSA activity/higher affinity for PBPs, sulfur linker is probably the key to this activity

  19. The Ceftaroline pyridine ring has what effect on the characteristics of this molecule?
    Makes the molecule a zwitterion making the drug poorly water soluble

  20. is this an active drug or a prodrug and why?
    Prodrug, because of phosphono group

  21. Why is this drug poorly water soluble?
    Because it is a zwitterion, see the N on the R2 rings and the COOH

  22. Which Ceftaroline structures impart anti-MRSA properties and why?
    Oxime (B-lactamase resistance) and 1,3-thiazole ring (high affinity for PBPs) and the sulfur linker

  23. How is this drug administered and why?
    IV because it is a zwitterion, so is poorly water soluble

  24. (True/False) Ceftaroline possesses coverage against pseudomonas aeruginosa.
    False

  25. (True/False) Ceftaroline can only be given intravenously.
    True

  26. (True/False) The 1,3-thiazole ring enables this agent to have activity against resistant gram-negative organisms.
    False

  27. (True/False) The 1,2,4-thiadiazole ring on ceftaroline increases the affinity for the transpeptidase enzyme
    True

  28. (True/False) Ceftaroline is a prodrug
    True

  29. (True/False) The sulfer linker, combining the 1,3-thiazole ring to the compound has no relation in making this agent contain anti-MRSA activity
    False, may be the key to its Anti-MRSA effects

  30. (True/False) The C3,4 double bond is essential for activity
    True

  31. (True/False) The parent compound of this drug contains antimicrobial activity
    False ceftaroline is a prodrug

  32. (True/False) The 1,2,4-thiadizole ring increases affinity for the transpeptidase enzyme
    True

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