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SAR Notes | PDF | Medicinal Chemistry | Biochemistry
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SAR Notes

The document discusses how pharmacokinetic studies can examine the absorption, distribution, metabolism, and excretion of drugs and drug interactions. It also mentions toxicity studies and structure-biodegradability relationships. Introducing or removing functional groups from a molecule's structure can significantly impact its biological activity.

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b23bb1011
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181 views3 pages

SAR Notes

The document discusses how pharmacokinetic studies can examine the absorption, distribution, metabolism, and excretion of drugs and drug interactions. It also mentions toxicity studies and structure-biodegradability relationships. Introducing or removing functional groups from a molecule's structure can significantly impact its biological activity.

Uploaded by

b23bb1011
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as PDF, TXT or read online on Scribd
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Pharmacokineticstudies can entail studying absorption distribution


metabolism and excretion ADME of a certain molecule
drug
Interactions
Dang Receptor Measuring binding constants

Modification of the drugs


Toxicity studies
Formulation
of chemical and physical properties

informative
Qualitative SAR
Derived from
continousdata
Derived from
Tonicity studies
non continous
forog
data
Yes No

osiingstitcarnity relationship

SBR Structure Biodegradability Relationship

Examples

Introduction or Removal of a Ring System


addition size increase in shape changes
effects are most
unpredictable
increasing size better fills the hydrophobic pocket

E t.gg fg
RoliphamContideporessant
dimetroxyphemes
3 co
butyholactam
than 3 3,4 dimethoxy
phenyl butyrolactam

a small ring substitute c c double bonds


Introduction of z
can significantly
improve stability

Eon's
1 Amino 2 phenylethene
Tranyleypromine

s memorise
activity
biological

I
x
activity
biological

addition or replacement g various


Here please note that the
can impact significant differences in the
functional groups

biological activities
Increaseinvolume
andhydrophobicityforativity
Arylorypropanolamine
Derivative of
am is
Fm inthisposition
favorable

I
H bonddonor
Insertiongas
electronegativeatom
y
40
systems like afavour
substituents with
Indole and
Imidazoloneare hydrophilic
groups
a functional
portion
at ortho favorable
are

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