Phase 1 functionalization
-introduction of small polar functional group
Phase 2 conjugation
-introduction of larger, polar group
prodrug
pharmacologically inactive compound that is converted to an active drug by a metabolic biotransformation
soft drug
a drug that uses metabolism to promote its excretion
more active
A prodrug can be in active form in the beginning, as long as it is ___ after metabolism.
hard drug
-compounds that contain structural characteristics required for activity (active) but are not susceptible to metabolism
enalapril
Which is orally administered, enalapril or enalaprilat?
carrier-linked prodrug
a compound that contains an active drug linked to a carrier group that is removed enzymatically
bipartite
comprised one carrier attached to drug
tripartite
carrier connected to a linker that is connected to drug
mutual
two, usually synergistic, drugs attached to each other
bioprecursor prodrug
a compound metabolized by molecular modification into a new compound, which is a drug or is metabolized further to a drug.
ethyl, propyl, butyl, phenyl
Which functional groups binded to the r2 of an ester will cause the reaction to fail?