Fluoroquinolones Flashcards
True or false
Topoisomerase II of mammalian cells is the same as the topoisomerase II in the bacteria
False
Topoisomerase II of mammalian cells is DIFFERENT from the topoisomerase II in bacteria.
Mammalian DNA is linear
Bacterial DNA is circular
Which of the following is not a bacterial resistnace to fluoroquinolones?
A. mutation of bacterial topoisomerase
B. Mutation of mammalian topoisomerase
C. insuffient accumulation of drug in bacteria
B
If a bacteria mutates gyrA gene, which of the following antibiotics won’t work?
A. beta-lactams
B. Protein synthesis inhibitors
C. cyclic peptide antibiotics
D. fluoroquinolones
D
Which of the following colors is the pharmacopohore required for activity?
A. Blue
B. Red
C. Black
A. Blue
Called a carboxy-4-pyridone nucleus
True or False
Reduction of the highlighed parts will cause interference with gyrase-DNA complexation
False
FQ will inactivate
if there is a substitution at C2 then there will interference with gyrase-DNA complexation
If there is substitution at the C2 carbon what features will the FQ have?
A. Increased antibacterial activity
B. Broadens activity
C. interferes with gyrase-DNA complexation
D. increased absorption
C. Increased with gyrase-DNA complexation
What does the F-group on the C6 Carbon do to the FQ?
A. Required for activity
B. Increases antibacterial activity
C. Increases absorption therefore activity
D. Broadens activity
B. Increases antibacterial activity
Increased cell penetration due to lipophilicity
What effects do the F in the C8 carbon have? (select all that apply)
A. photosensitivity
B. Increases antibacterial activity
C. Increases absorption therefore activity
D. Broadens activity
A,C
The group C8 can be substituted with a -OCH3. What does the -OCH3 do for the structure?
A. Better Absorption
B. Improved antibacterial
C. Decreased photosensitivity
D. Adverse side effects
C
At the C7 position there can be a hterocyclic ring, what is the purpose of the heterocyclic ring?
A. Better absorption
B. Photosensitivity
C. Improved antibacterial effect
D. Produces CNS effects
C.
Which of the following statements is true?
A. Piperazinyl ring has the best antibacterial effects, but it has CNS effects
B. Piperazinyl ring decreases CNS effects
C. Alkyl substitutions on the piperazinyl ring increase CNS effects
D. alkyl substiution on piperazynyl ring decrease CNS effects
A, D
Adding a cyclopropyl ring to the N-1 position does which of the following?
A. Improves antibacterial Activity
B. broadens activity
C. Increased CNS effects
D. Decreases CNS effects
B. Broadens Activity
The following structure covers what type of bacteria?
A. Gram Positive
B. Gram Negative
C. Atypical
D. A and B
E. B and C
F. All of the above
F. All of the above
Atypical bacteria have no cell wall examples include chlamydia, mycoplasma, and legionella
A third ring in the nucleus does what to the FQ?
A. Produces CNS effects
B. Increases Photosensitivity
C. Increases Absorption
D. Increases Activity
D
What activity does the highlighed arrow have?
A. Increased Activity
B. interferes with gyrase-DNA complexation
C. Increases photosensitivity
D. Increased absorption
A. Increased antibacterial activity
Which of the following statements is true about the arrow pointing at Norfloxacin? (select all that apply)
A. Alkyl susbtitution on piperazinyl ring increases CNS Effects
B. Piperazinyl causes CNS effects
C. piperazinyl decreases CNS Effects
D. Alkyl susbtitution on piperazinyl ring decreases CNS Effects
B, D