PRESENTATION ON

DIAGNOSTIC AGENT
Subject: Medicinal cheemistry ii (PHC-807)
Faculty: pharmaceutical chemistry
By alveena sadiq.
Content
 Introduction
 Classification
 Preparation
 SAR
 Mechanism of Action
 Innovtion
Introduction of Diagnostic agent;
 Definition:
 Diagnostic agents are group of techniques often used in the diagnosis and
subsequent treatment of disease.

Basically these are chemical compounds of inorganic and organic in

nature

used to detect abnormalities in the tissue structure and to check

defective functioning of body organ

It do not have medicinal & pharmacological effect

Classification

Broadly we can divide the various

compounds used as a diagnostic
agent into four major classes as

 Inorganic Compounds
 Dyes and stains
 Culture media or
chemical basic
constituent being
AGAR.
 Radiopharmaceuticals
1.Inorganic compound:
Inorganic compounds are drugs and diagnostic agent ,it focuses on
area of demonstrated medical and clinical interest.
There are several inorganic compound that are use for diagnosis purpose; some are listed below .

SAR:
USE:
In its crystal It is
structure each  also used as a
INTRODUCTIO citric acid
N positive oral
 moiety has lost contrast agent in
: Ferric  four protons, magnetic
ammonium cit and the resonance
rate deprotonated imaging, and
 is a yellowish hydroxyl groups was formerly
brown to red act as ligands administered
solid with a together with orally as a
faint odor of  four carboxylate source of iron
ammonia. It is groups; two for the
soluble in  carboxylate treatment of
groups are not iron-deficiency
water.  coordinated to Figure 1: structure of
anaemia. ferric ammonium
the ferric ion. citrate
 Aminohippuric acid Aminohippurate is These are compounds

Mechanism of Action:
introduction
or para- filtered by the renal containing hippuric
aminohippuric acid glomeruli and acid, which consists
(PAH), a derivative secreted into the of a of a benzoyl
of hippuric acid, is a urine by the proximal group linked to the
diagnostic agent tubules. By N-terminal of a
useful in medical measuring the glycine.
tests involving the amount of drug in
kidney used in the the urine it is
measurement of possible to
renal plasma flow. determine functional
capacity and
effective renal
plasma flow.

it belongs to the class

of organic compounds
known as hippuric
acids.
 There are several dyes and stain that used in
laboratories for identification of compound:

2. Dyes And
Stain

Dyes are Solutions that

color or mark tissue for
identification and staining
agents that react
differently with abnormal
cells than with normal
cells
CONGO RED Properties
• It is an Azo dye.
• Congo red is water-soluble,
yielding a red
colloidal solution; its
solubility is greater in
NOMENCLATURE: organic solvents.
• formula:
3,3′-([1,1′-biphenyl]- C32H22N6Na2O6S2;
molecular weight: 696.66
4,4′-diyl)bis(4- g/mol.
aminonaphthalene-1- • The Color Index Number of
CR is 22120
sulfonic acid) • CR has the property to
change the color from blue
to red at pH 3.0–5.2 .
USES:
used as biological stain
as diagnostic
aid(amyloidosis).
Figure:2 structure of
Congo Red
Structure activity
relationship
1.CR is the sodium salt of
benzidinediazo-bis-1-
naphtylamine-4-sulphonic
acid .
2. Congo red has two azo
bonds (-N=N-) and this
bond responsible for
metachromatic property.
3.Hydrophillic interaction
between aromatic ring
lead to pi-pi stacking
which also increase
activity.
 Classification
3. Culture media
chemical

AGAR:
 Agar is gelatin like material
chemically related to
carbohydrates, which is used as a
base for culture media for growing
bacteria.
 Agar is a mixture of two
components: the linear
polysaccharide agarose, and a
heterogeneous mixture of smaller
molecules called agaropectin.
Structure Activity Relationship
 Agar  can be considered to consist mainly of
alternating β-(1-3)-D and α-(1-4)-L linked
galactose residues.

 Most of the α-(1-4) residues are modified by

the presence of a 3,6 anhydro bridge.

 The other modification that can be found are

mainly substituents of sulphate, pyruvate,
uronate or methoxyl groups.

 Modern alkalie treatment methods tend to

increase the level of anhydro bridging in the
molecule which subsequently improves the gel
strength.

 The level of methoxy content appears to be one

of the main structural moieties that determines
the gel setting temperature with very low
methoxy contents giving the lower setting
Figure 3: structure of Agar.
Applications

 Isolation, identification
(with the use of either 
Optochin disc or 
Bacitracin disc and testing
the sensitivity of the
isolate)  and antimicrobial
susceptibility of
Streptococci.
 Determine the type of
hemolysis, if any by using
Blood Agar. 
Radiopharmaceuticals:
Radiopharmaceuticals are
radioactive labelled substances
containing one or more
radionuclide(s) suitable for
administration to humans
The chemical and physical properties
of the radiopharmaceutical affect its
localization in the body, while the
radioactive decay properties
determine the detection method and
the diagnostic or therapeutic
applicability
Factors that often determine t
. he usefulness of
diagnostic agents are:
1.The ideal contrast agent
(radiopaque) should have
Ready availability and low cost
2.Excellent x ray absorption
3. chemical composition
(stability)
4.Solubility(high water
solubility, low viscosity)
5.The ability to be
administered for selective
tissue uptake and excretion
6.Minimal toxicity (minimal
osmotic effect)
 Radioactive decays

BASIC TTERMINOLOGY

 Isotopes
Atoms of the same element with
different atomic mass numbers numbers
e.g. carbon-12, carbon-13 and carbon-
14
Nuclideis
a type of atom whose nuclei have
specific numbers of protons and
neutrons
Notation of a nuclide= EZ
e.g. = 235U92 e.g. = 235U92 12/26/12 7
All Article Types
Mechanism of Action
of
Radiopharmaceutical


 The radiopharmaceutical is the
result of the linkage of two
elements, a carrier and at least
one radioactive atom that, with
its nuclear properties, defines
the diagnostic and/or therapeutic
nature of the radioactive
compound. The carrier plays an
important role in the selective
transport of the radionuclide to a
specific biological target (Figure
4) Figure 4. Schematic representation of linkage of the
carrier and the radioactive atom to form the
radiopharmaceutical that interacts with a specific
biological target.
Some
medically
use Radio
isotopes
 Introduction
• Iodine is in group VIIB with the other halogens (fluorine, chlorine,
bromine, and astatine).
Radiochemistry • iodine are known with at least five different oxidation states;
of however, in nuclear medicine, the —1 and+1 oxidation states.
• The -1-oxidation state represented as sodium iodide (NaI) is important
Iodine
for thyroid studies
• The useful radioisotopes of iodine for organ imaging are iodine-123
USES and iodine-131.
The major indications
for thyroid imaging with
sodium iodide (123I) are
for evaluation of thyroid
SAR
function (uptake) and/or • The electrophilic species (I+ ) can be generated from iodide
morphology (imaging).
(I-) by various oxidizing agents, including (a) chloramine-T
(N-chloro-p-toluene sulfonamide) sodium, (b) enzyme
oxidation of (lactoperoxidase), and (c) Iodo-Gen (1,3,4,6-
tetrachlora- 3-6-diphenylglycoluril).
Prparation
• Iodine-123 is produced in a cyclotron by
bombarding a xenon-124 target with a proton
according to the 124Xe (p,2n)123 Cs→123 Xe→ 123I
sequence. Figure:5 Working
• Iodine-123 is isolated in the iodide form. Diagram
• 123I has a half-life of 13.22 hours, decays through
EC and emits γ-rays, making 123I useful for
imaging.
 The most commonly Tc/Re The chemistry of

CLASSIFICATION

SAR
INTRODUCTION
used radioisotope of radiopharmaceuticals are technetium is similar to
technetium is tech- classified into three that of rhenium and is
Radiochemistry of generations. dominated by forming
netium-99m, which is
Technetium-99m produced by compounds by bonding
between the electron-
molybdenum-99 þ—
(99mTc) decay in a
1.1st Generation: Known
as Tc/Re Essential. Less
deficient metal and
electronegative groups,
molybdenum- target specific and which are capable of
99/technetium-99m generally used as donating electron pairs.
The name is derived generator. perfusion agents. Some examples of these
from the Greek Technetium, is a electronegative groups
transition state metal 2.2nd Generation: include amines,
‘tekhnetos’, meaning carboxylic acids,
and is the only “ar- Contains a bifunctional
artificial.1 It was tificial” element with a chelator whose function hydroxyls, isonitriles,
discovered by Emilio lower atomic number is to chelate to the metal oximes, phos- phates,
and have a targeting phosphines, and
Segre and Carlo Perrier than uranium. No
moiety. sulfhydryls. Various
stable isotopes exist in oxidation states (e.g.,
in 1937 in Italy. nature. +1, +3, +5, etc.) are
3.3rd Generation: Uses prepared in the
USES: the integrated approach. presence of the
The targeting moiety of reducing agent and
Is also used as a tracer the pharmaceutical is stabilized by
in medicine. It deposits directly bonded to the complexation with
metal. available ligands.
in the brain, liver,
kidneys, spleen, and
bones to diagnosed
diseases.
Figure 3. Inorganic technetium functional
groups useful for labelling bioactive
molecules. HYNIC=6-
hydrazinonicotinamide.
Preparation
 Technetium-99m radiopharmaceuticals are
prepared by combining sodium
pertechnetate (Na99mTcO4) with nonra-
dioactive components in a sterile reaction
vial. The primary chemical substances in
the vial are the complexing agent (ligand)
and a stannous salt-reducing agent
(stannous chlo- ride, stannous fluoride, or
stannous tartrate). The oxidation state of
technetium in various complexes as well as
the actual chemical structure of many
radiopharmaceuticals has yet to be
characterized.
 After preparation of the
radiopharmaceutical, tests for ra-
diochemical purity should be carried out to
ensure that the radiotracer is in the correct
radiochemical form. Analytical quality
control methods include paper and thin-
layer chro- matography, column
chromatography, and solvent extrac- tion
 Example of Technetium:
•99mTc exametazime-99mTc exametazime-
cerebral perfusion
• 99mTc macroaggregated albumin used Pulmonary
perfusion
• 99mTc medronate- bone imaging
• 99mTcpertechnetate-- imaging of thyroid,&
salivary glands.

Procurement & Storage:

Because of the short life of the radiopharmaceuticals the nuclear
pharmacist will order the drug directly from manufacturer usually
through over night delivery •
In addition knowledge of calibration time shipping/delivery schedules
and radio active decay associated with the ordered radio schedules
pharmaceutical weigh heavily in the ordering process
isotope storage areas should be as per the rules. there should be a
separate lab for the manipulation and preparation of radio
pharmaceutical dosage and another for calibration of doses.
Scientists Develop New Laser That Can Find and Destroy Cancer Cells in the Blood
By Yasemin Saplakoglu June 15, 2019
Originally published on Live Science & NCI
 

 The new technology, dubbed the Cytophone, uses

pulses of laser light on the outside of the skin to
heat up cells in the blood. But the laser only
heats up melanoma cells — not healthy cells —
because these cells carry a dark pigment called
melanin, which absorbs the light. The Cytophone
then uses an ultrasound technique to detect the
teensy, tiny waves emitted by this heating effect.
Conclusion:

 Diagnostic agents are chemical compound which are specific in their reactions
by which definite conclusion may be drawn in both cases either in term of
qualitative and quantitative regarding the cause of disease itself
 These compounds are helping aids for clinical pathology in general and other
branches of medical science.
 Diagnostic radiopharmaceuticals are a powerful tool in the diagnosis of
cancer, cardiological disorders, infections, kidney or liver abnormalities, and
neurological disorders.
 Newer radioactive isotopes,dyes and compounds are providing to be modern
diagnostic agents.
 The more the disease,more the diagnostic agents are to be required.
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Chemistry ,edition 12,  LWW; Twelfth, North American edition (March 2, 2010)
 Katja Dralle Mjos and Chris Orvig*,2014, Metallodrugs in Medicinal Inorganic Chemistry,journal of
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 Yen Wang, Editor, CRC Hand book of Radioactive Nuclides, (The Chemical Rubber Co., Cleveland,
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  Agar Archived October 16, 2007, at the Wayback Machine at lsbu.ac.uk Water Structure and Science