What is statine?Non-natural amino acid Non-natural amino acid contained within
contained within pepstatin.
pepstatin.
Pharmacore
The portion of a molecule that determines the biological effects of a drug
Methylene
Hydrophobic contributor used to increase chain/ring size and make it easier
to cross membranes.
Aromatic
Type of ring that cannot be added to.
Increased
Effect of DB on metabolism of a drug.
Double Bonds
Used to change degrees of unsaturation.
Decreased
Effect of double bonds on flexibility.
Increased
Effect of double bond on potency of an
analogue.
Hard drug
Resistent to metabolism
Soft drug
Predictable and controlled metabolism
Hard handle
Added to decrease a drug's metabolism.
Stereocentre
C-atom must be sp3 hybridised and have
four different substituents.
LogP
Partition coefficient.
5
Lipinski's rules - H-bond donors.
500
Lipinskis rules - molecular weight.
5
Lipinskis rules - LogP
10
Lipinskis rules - H-bond acceptors
10
Lipinskis rules - rotatable bonds.
pKa
The pH at which the ratio of the molar
ratio of a drug's acid to its conjugate base
is 1:1.
pH>pKa
pH/pKa relationship where there is increased conjugate base formation.
pH
Structure - Activity Cheat Sheet
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