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PC2 Chemistry of Fluoroquinolones
Terms in this set (18)
What is the MOA of fluoroquinolones?
Inhibition of DNA synthesis by targeting DNA gyrase and topoisomerase IV
Are fluroquinolones bactericidal or bacteriostatic?
What is the spectrum of activity of fluroquinolones?
What is the basic core structure of fluoroquinolones?
What part of the molecule is responsible for potency?
What part of the molecule is responsible for spectrum of activity?
What part of the molecule is responsible for cell wall penetration; potency?
Which was the first FQ active outside the urinary tract?
Which FQ was withdrawn from use due to hemolysis and renal failure?
Which FQ was withdrawn from use due to liver toxicity?
Which FQ was withdrawn from use due to cardiovascular toxicity and sudden death?
Which FQ was withdrawn from use due to excessive phototoxicity?
temafloxacin and sitafloxacin
Analogues with a C-8 chloro group were identified as very ________?
Which enzyme introduces supercoils into DNA?
Which enzyme functions to remove knots that accumulate in the chromosome?
What facilitates quinoline-topoisomerase binding?
facilitated through a water-metal ion bridge
FQs kill bacterial cells by __________ the concentration of of enzyme-DNA cleavage complexes
What are the resistant mechanisms involving FQs?
•Mutations in gyrase and topoisomerase IV
•Increased efflux pumps
•Enzyme inactivation (AAC)
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