Chem Basis - AGNs 4

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Chem Basis - AGNs 4
2014-02-11 18:48:54
Chem Basis AGNs
Chem Basis - AGNs 4
Chem Basis - AGNs 4
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  1. Is Amikacin susceptible to aminoacetyltransferase?
    Yes, acetylates the 6''-amino group
  2. Which AG ring is the primary target for bacterial inactivating enzymes?
    • Ring I

  3. Is Ring 1 essential for activity?
  4. Can you describe an aminoglycoside as a aminoglycosidic aminocyclitols, why or why not?
    Yes, they have an aminocyclitol ring glycosidically linked to cyclic amino/sugars
  5. What is classification of Aminoglycosides based on?
    Type of aminocyclitol substitution pattern
  6. What are the two pharmacophores for AGs?
    • 1)  Streptadine: a diguanidine derivative of a 1,3-diaminohexose (e.g. Streptomycin). 
    • 2)  2-Deoxystreptamine: 1,3-diaminocyclohexane. (Amikacin, Neomycin and Tobramycin)
  7. Which AGs are 2-Deoxystreptamines?
    Amikacin, Neomycin and Tobramycin
  8. Which AGs are Streptadines?
    • Streptomycin
  9. What are the different types of 2-Deoxystreptamines?
    • 1) Substitution on 4 and 5 hydroxyl groups 
    • 2)  Substitution on 4 and 6 hydroxyl groups
  10. The nature of the diaminocyclohexane group impacts what characteristics of the molecule?
    • Chemistry
    • Spectrum
    • Potency
    • Toxicity
    • Pharmacokinetics
  11. Streptadine derivatives are mainly used for what?
    • Tuberculosis
  12. The lack of 2-OH group on the 2-Deoxystrempamine derivative, has what effect on the AG?
    • Increases resistance
  13. Which of these sugars can be substituted on the 2-DOS or Streptadine pharmacophore of AGs and maintain resistance: glucosamine, dextrose, ribose, deoxyribose or streptose?
    • Glucosamine, ribose and streptose
  14. The polar -OH groups and amino groups on AGs may contribute to the high polarity, how do you expect that they are excreted?
    In the urine
  15. Are AGs water or lipid soluble?
    Water soluble at all pHs
  16. Do AGs form base or acid addition salts and why
    They are basic so they form acid addition salts
  17. Are AGs usually excreted in the active form in the urine?
  18. Is Neuromuscular blockade is a side effect associated with AG?
  19. Are AGs potentially a good choice in a patient with allergy to penicillins?
  20. What is the main mechanism of inactivation of AGs?
    Enzymatic inactivation