Chem Basis CPN structures 3

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    What CPNs have are cephamycins?
    Cefoxitin and Cefotetan
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    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
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    Compare the G+ coverage of these two drugs:
    Cefepime has greater G+ coverage because it is less polar, see the R’ substituents
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     Is cefepime a good choice for treatment of a bacterial infection that is resistant to Ceftazidime and other 3rd gen CPNs?
    Yes
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    How do these two drugs compare in B-lactamase resistance?
    Cefepime has greater B-lactamase resistance
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    (True/False) An ester for the carboxylic group produces an active drug with enhanced absorption.
    False, it would not be active
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    (True/False) methoxy at -C7 produces cephamycin series with enhanced beta-lactamase resistance.
    True
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    What is this drug?
    Ceftaroline
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    Ceftaroline is known for what special spectrum enhancements?
    Expanded G+ coverage to include Staph aureus and streptococcus pneumoniae
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    Does Cefaroline’s spectrum cover P. auruginosa?
    No
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    Does Ceftaroline have a larger G- spectrum than other CPNs?
    No, similar G- coverage
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    The Ceftaroline phosphono group has what characteristics?
    Increases solubility (not present in activated drug)
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    The Ceftaroline 1,2,4 thiadiazole ring has what characteristics?
    Good G- penetration and transpeptidase activity due to its polarity
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    The Ceftaroline Oxime group has what characteristics?
    Enhances B-lactamase resistance
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    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
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    The Ceftaroline pyridine ring has what effect on the characteristics of this molecule?
    Makes the molecule a zwitterion making the drug poorly water soluble
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    is this an active drug or a prodrug and why?
    Prodrug, because of phosphono group
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    Why is this drug poorly water soluble?
    Because it is a zwitterion, see the N on the R2 rings and the COOH
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    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
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    How is this drug administered and why?
    IV because it is a zwitterion, so is poorly water soluble
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    (True/False) Ceftaroline possesses coverage against pseudomonas aeruginosa.
    False
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    (True/False) Ceftaroline can only be given intravenously.
    True
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    (True/False) The 1,3-thiazole ring enables this agent to have activity against resistant gram-negative organisms.
    False
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    (True/False) The 1,2,4-thiadiazole ring on ceftaroline increases the affinity for the transpeptidase enzyme
    True
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    (True/False) Ceftaroline is a prodrug
    True
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    (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
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    (True/False) The C3,4 double bond is essential for activity
    True
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    (True/False) The parent compound of this drug contains antimicrobial activity
    False ceftaroline is a prodrug
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    (True/False) The 1,2,4-thiadizole ring increases affinity for the transpeptidase enzyme
    True

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Author:
kyleannkelsey
ID:
258476
Filename:
Chem Basis CPN structures 3
Updated:
2014-01-28 21:31:18
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Chem Basis CPN structures
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Chem Basis CPN structures 3
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