Cushman Flashcards
Production of Sulfanilamide
Prontosil is broken down by bacteria and creasted sulfanilamide
Structure relationship
the attachement of electron withdrawling heteroaromatic rings acidified the sulfonamide nitrogen and enhanced the potency
Increase acidity is due to the electronegativity of the aromatic substituent
The increase in acidity also decreases the incidence of crystalluria
DHFR gene mutation
bears mutation that enables the expressed enzyme to be active in the presence of drug through a decreased binding affinity of trimethoprim
Metabolism
Metaboloized by N-4 N-acetylation and in some cases N-1 Glucuronidation
Colistin
Contains 2,4-diaminobutanoic acid residues that are protonated at physiological pH