History

medicinal Chemistry
a chemistry based discipline , involving aspects of the
sciences
biological , medicinal and pharmaceutical

It is concerned with the invention

discovery design identification
,

and prep of biologically

active compounds the study of their metabolism
,

the interpretation of their wide of action at the molecularler e

and the construction of structure activity relationship

Ned Chem covers :

Stage
:Neuactivesubstan ordrugareda
1

ran or
as lead
biotechnological
molecules
processes They
.
are known

2 :

Optimization stage
3 :
Developmental stage
-optimization of sythethic route for bulk production
andmodificationpanpharmaceutic propertiea
General Steps In the discovery of
disease state
New
drug for aspecific
 study obj of med chem
Physio chemical properties of ding molecules
in relation to ADME
dulg
chemical basisof pharmacology and therapeutic
Fundamental pharmacophores for dings used to treat
disease
structure activity relationships in relation to
drug target
interactions
chemical pathways of drug metabolism
Application to making drug theraphy decisions

History and Development of Med chem

Drugs of antiquity
-

8000 BC : Prehistoric medicine

care paintings

2000
Egyptian medicines
BC :
-

goddess Shechmet
papyrus
·

obstetrics gynecologists
·

2000 B2
showrung
>
chang shang and mahuang
-

450BU to 300AD Greeks and Romans

:

Hippocrates father of modern Medicine Appocratic Oath

· -

homans
 the middle Ages
500 1400 AD The Middle Ages
:

700 -
1500 AD :
Arabic medicines

1700 -

1900 (18-19th centuries

Industrial revolution

19th century :
Age of Innovation Chem
and

the 20th century and the Pharmaceutical Industry

21st centriny

important techniques used in Drug development and

medicinal chemistry
 Unit 11 :
Physicochemical Properties of Drunge
Drug
gives therapeutic action
-

Dung Product
-

with packaging
as a whole

Biopharmaceutics
:

Absorption
transfer of Drug from site of admin. to site of action
/BloodStreamla
>
-

a
A

-Drug Disposition
Elimination
Broavailability
Measure a absorption
>
-
 protein-nucleicacid
molecule enzymes
Pharmacodynamicsainteraction
·
·

rug-Receptor
=
Therapeutic Action

Affinity
Primary ligand released
indigenous substances by body
Normal Response
·

~
Normal epinephrine
Agonist
Administer similar to primary ligand like epinephrine
primary ligand
Follows
Antagonist no response neutral no effect
blocks receptor =
response , ,

Inverse Agonist
Chapter 3
Joge next lesson

chemical/physicaltributes of drags affecting drug action

targetting target site
Minor changes in lead structure
change in the size and shape

SAR studies
chemical compound
-I screening
Lead molecule
↓ Pruning/optimization
Pharmacophore
Pruni

Sar p . 296

Remington chapter 28
have common name activity
generic name
Analgesics
-

Drugs that bring about insensibility

to pain without

who has lower pain tolerance ?

Male
·
viscous solution
195 % conc
, not soluble in H20
 due to oxidation

oxidized

·
ideal as
pharmacetical product
>
-
foul swelling
 -

-
C-
- for get
-

?
for fluid
with force liquid
who force viscous
> for hair
-
waves
 superdisintegrants
-

>
-
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 suha
- shaddock, citrus maxima
, biggest
-

hybrid of
sulat
mandahin
calamonin

sweet -

honey orange