GMS 6504 CHAPTER 4 Questions With Complete Solutions
what makes a good drug vs a bad one
- Lipinski's Rule of 5
- Chemical reactivity: good or bad?
- Some chemically or biologically reactive functional groups to
recognize
- Choosing a target
lipinski's rule of 5
poor absorption or permeation of drug are more likely when,
1.Molecular mass greater than 500 Da
2.High lipophilicity (expressed as LogP greater
than 5)
3.More than 5 hydrogen bond donors
4.More than 10 hydrogen bond acceptors
partition coefficient
The ratio of the equilibrium concentrations of a dissolved
substance in a two-phase system containing two largely
immiscible solvents (water and n-octanol)
improvements on the Lipinski parameters
1. Partition coefficient log P in -0.4 to +5.6 range
2. Molar refractivity from 40 to 130
3. Molecular weight from 160 to 500
, 4. Number of atoms from 20 to 70 (includes H-bond donors
[e.g.;OHs and NHs] and H-bond acceptors [e.g.; Ns and Os])
5. Polar surfa
size comparison of CNS vs NCNS drugs and why
- CNS drugs are smaller compared to NCNS drugs
- Blood brain barrier has to be crossed, thus smaller molecules
are permeable across
explain how chemical reactivity determines if a drug is good or
bad
1.Modification of Proteins and/or Nucleic Acids(Bad if
unanticipated and non-selective, but can be good if selective)
2. Labile in Biological Systems *Esters
*Amide Bonds
*Disulfide Bonds
Bad (Compound may be degraded in vivo); Good (Can be
incorporated into the design of pro-drugs)
example of chemically reactive functional group
michael acceptors which contain carbonyl groups and adjacent
conjugated double bonds
Sometimes drugs are designed to make use of metabolic
processes in order to generate their active form, example is by
adding promoiety which allows to cross the barrier. what is the
reason
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