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28. Antimicrobial Drugs - Part 4 of 5
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Problem 11
28. Antimicrobial Drugs - Part 4 of 5
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28. Antimicrobial Drugs / Inhibitors of Cell Wall Synthesis: Beta-lactam & Penicillin / Problem 1
Problem 1
Why is the beta-lactam ring essential to the activity of beta-lactam antibiotics?
A
Because it acts as a rigid hydrophobic anchor that inserts into the cytoplasmic membrane and blocks nutrient transport channels essential for cell viability.
B
It chelates divalent metal cofactors in autolytic enzymes causing those enzymes to hyperactivate and digest cell wall components independent of PBPs.
C
It mimics the D-Ala-D-Ala substrate of PBPs, enabling covalent binding and inhibition of the cross-linking enzymes; cleavage of this ring by beta-lactamase abolishes activity.
D
Because it is the principal determinant of oral bioavailability by protecting the molecule from first-pass hepatic metabolism, explaining why versions without it are rapidly cleared.
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