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Drug molecules that mimic peptides.
Peptidomimetic class where R groups are bound to N.
Drug interaction w/ target.
Absorption, distribution, metabolism, excretion (ADME).
High lipophilic molecule issues
- 1) Low water solubility
- 2) Easily metabolized
- 3) Bind excessively to plasma protein
- 4) Can build up in tissue
Low lipophilic molecule issues
Poor membrane solubility.
- a = ________ of compound in ________
LogP value meaning
- <0 = injection
- 0-3 = oral administration
- 4-5 = transdermal application
- <5 = toxic issue due to build up in tissue
Shake Flask Measurements
- 1. Put compound in flask with octanol and water.
- 2. Shake
- 3. Measure solubility using UV-vis, GC/MC, HPLC
Lipinski's Rule of 5
Came from sabermetrics
- 1. Not more than 5 HBD
- 2. Not more than 10 HBA
- 3. MW < 500
- 4. LogP < 5
- LogP of ionizable compound at pH n.
- D stands for distribution.
pKa relation to pH
if pH = pKA, 50% base and 50% acid form of compound. if pH > pKa, more in acid form, if pH < pKa, more in basic form.
Drug Efficiency requirements
Drug must be polar enough to be aqueous soluble and lipophilic enough to pass membrane.
Altering pKa of compounds
Adding electron withdrawing or donating species to compound.
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