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GMS6504 #2 Exam Questions With Complete Solutions
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GMS6504 #2 Exam Questions With Complete Solutions
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GMS6504 #2 Exam Questions With Complete Solutionswhat are the four things that make a good drug versus a bad
one?
1. Lipinski's Rule of 5
2. Chemical reactivity: good or bad?
3. Some chemically or biologically reactive functional groups to
recognize
4. Choosing a target
explain the old lipinskis rule of 5 and the rules
Poor absorption or permeation are more likely when:
1. Molecular mass greater than 500 Da (want small and
absorbable)
2. High lipophilicity (expressed as LogP greater than 5) (often
contributes to high metabolic turnover, low solubility, and poor
oral absorption. In addition, highly lipophilic compounds tend to
bind to hydrophobic targets other than the desired target, and,
therefore, there is an increased risk of promiscuity and toxicity.)
3. More than 5 hydrogen bond donors (OH, FH, NH: no more
than 5)
4. More than 10 hydrogen bond acceptors (want no more than
10)
define the 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)
(refers to if the molecule prefers to be in water or oil)
what is the partition coefficient equation?
P= (C oct / C water)
For the partition coefficient equation; part of the equation must
change in order to be used in real life and why is this?
Log P = (C oct / C water)
Since the differences are usually on a very large scale, Log10(P)
is used. (usually is between 0 and 10)
,what are the improved lipinski parameters ? (aka what they
actually use now in pharmacology)
1. Partition coefficient log P in -0.4 to +5.6 range ( means a very
large amount in 1-octanol and not a lot in water)
2. Molar refractivity from 40 to 130 (It represents size and
polarizability of a fragment or molecule.)
3. Molecular weight from 160 to 500 Da (so not toooo small but
def not too big)
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])
(refers to weight too)
5. Polar surface area no greater than 140 Å2 (once again not too
big)
, explain the difference between CNS and NonCNS drugs and
what trend/ why there is a difference
CNS wants smaller drugs, smaller polar surface area, this is due
to the fact that CNS drugs must pass through the BBB
explain the good and bad sides of chemical reactivity when it
comes to drug design
1.Modification of Proteins and/or Nucleic Acids (bad b/c if its
over modified cant be fixed and have to wait for body to make
new protiens ect.) (Bad if unanticipated and non-selective, but
can be good if selective)
2. Labile in Biological Systems (how it breaks down in the
body/ a compound that undergoes reactions with a relatively
high rate of. substitution.)
- can be substitutions of Esters Amide Bonds *Disulfide Bonds
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