mevastin
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prodrug: structure that gets opened in the body
when drug hits blood or liver enzymes cut the bond between C in ring and
O to get open CO2 on one end and OH on the other end
Role of Water in this rxn
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, 1. base steals H from water.
2. C=O double bond breaks into single bond
3. electrons from H2O attack carbocation from (2)
4. O reforms double bond
5. O on enzyme steals back H and the rest of the molecule leaves
Chain extension/contraction
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vary linker size to optimize interactions (binding) of groups
at two ends
add of remove carbon atoms
B-lactamase destroys antibiotics
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penicillin + B-lactamase = non functional penicillin
Cephalosporins
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, inhibit cell wall synthesis
very lipohilic
has a [4,6] ring which is less reactive than a [4,5] ring.
therefore this drug has a lower risk of allergy and higher
activity against resistant strains
low potency meaning requires a high dose
not orally active
Clavulanic acid destroys B-lactamase
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Clavulanic acid + b-lactamase = non functional enzyme
phosphorylation of acyclovir
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viral enzyme will add 1 phosphate to the end of the drug.
once the enzyme is phoshphorylated, the human enzyme
can now accept the substrate and add 2 more substrates
HIV resistance
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HIV replicated rapidly (10billion per day)
anti HIV agents select resistant strains unless all viral proliferation is
blocked
no single anti HIV agent can do everything
Cross-link formation
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on each D-amino acid there is a CO2H side chain where the
peptide bond forms
Where does cholesterol come from?
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Diet and liver (saturated and trans fat)
excess cholesterol stored in arterial walls (plaque)
Immunization
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Give this one a try later!
prodrug: structure that gets opened in the body
when drug hits blood or liver enzymes cut the bond between C in ring and
O to get open CO2 on one end and OH on the other end
Role of Water in this rxn
Give this one a try later!
, 1. base steals H from water.
2. C=O double bond breaks into single bond
3. electrons from H2O attack carbocation from (2)
4. O reforms double bond
5. O on enzyme steals back H and the rest of the molecule leaves
Chain extension/contraction
Give this one a try later!
vary linker size to optimize interactions (binding) of groups
at two ends
add of remove carbon atoms
B-lactamase destroys antibiotics
Give this one a try later!
penicillin + B-lactamase = non functional penicillin
Cephalosporins
Give this one a try later!
, inhibit cell wall synthesis
very lipohilic
has a [4,6] ring which is less reactive than a [4,5] ring.
therefore this drug has a lower risk of allergy and higher
activity against resistant strains
low potency meaning requires a high dose
not orally active
Clavulanic acid destroys B-lactamase
Give this one a try later!
Clavulanic acid + b-lactamase = non functional enzyme
phosphorylation of acyclovir
Give this one a try later!
viral enzyme will add 1 phosphate to the end of the drug.
once the enzyme is phoshphorylated, the human enzyme
can now accept the substrate and add 2 more substrates
HIV resistance
, Give this one a try later!
HIV replicated rapidly (10billion per day)
anti HIV agents select resistant strains unless all viral proliferation is
blocked
no single anti HIV agent can do everything
Cross-link formation
Give this one a try later!
on each D-amino acid there is a CO2H side chain where the
peptide bond forms
Where does cholesterol come from?
Give this one a try later!
Diet and liver (saturated and trans fat)
excess cholesterol stored in arterial walls (plaque)
Immunization
Give this one a try later!
