CH450 INORGANIC CHEMISTRY

Mentor: Dr. Kabaso Kalebaila

Email: kkalebai@gmail.com
School of Mathematics and Natural Sciences
Chemistry Department
 Medicinal Compounds
Medicinal Inorganic Chemistry is an interdisciplinary research area
incorporating different branches of chemistry and biology in the
research for better and new drugs.

Medicinal Inorganic Chemistry: deals with the discovery and design of

new and better therapeutic chemicals and development of these
chemicals into new medicines and drugs.

Generally Medicinal Chemists can:

• Make new compounds

• Determine their effect on biological processes.
• Alter the structure of the compound for optimum effect and
minimum side effects.
• Study uptake, distribution, metabolism and excretion of drugs.
 Inorganic Medicinal Compounds
• During the 1840s, the first use of synthetic organic chemicals
were nitrous oxide, ether, and chloroform as anesthesia during
a tooth removal.

• In 1864, barbituric acid was synthesized as a useful hypnotic.

• In 1875, salicylic acid was introduced as a possible cure for

typhoid fever. It was found to be an effective antipyretic.
 Medicinal Compounds
In 1898, the first commercially available semisynthetic
morphine was introduced as a cough sedative.

In 1899, Aspirin (acetylsalicylic acid) was marketed as an

painkiller without the unpleasant side effects.

Medicinal Chemistry began.

 Inorganic Medicinal Compounds
Inorganic Medicinal chemistry is concerned with the development
and application of inorganic compounds in medicine

There are two types of inorganic medicinal agents namely

a) Diagnostic Agents

b) Therapeutic Agents

 Diagnostic is a process of distinguishing symptoms. The chemicals

used to distinguish symptoms are known as diagnostic agents. These
could be inorganic or organic based.

 Therapeutic Agents: are used in the treatment of disease or

disorders in the organism.
 Inorganic Medicinal Compounds
a) Diagnostic Agents
 Diagnostic agents are the substances used to examine
the body in order to detect impairment of its normal
functions.

Usually these agents find no other use in medicine.

Diagnostic agents are divided according to the use such as:

• drugs used as radiation contrast media

• drugs used to test organ functions
 Inorganic Medicinal Compounds
a) Diagnostic Agents

What is Diagnostic Imaging?

• A field of medicine used in determining physiology,
managing disease, and locating abnormalities in the body.

Diagnostic Techniques
• X-Ray Imaging
• CAT or CT Scans
• Ultrasound Imaging
• Magnetic Resonance Imaging
 Inorganic Compounds in Medicine: Examples

In X-Ray Imaging
• Was the first “Great Discovery” in the field of
diagnostic imaging
• Wilhelm Roentgen discovered that a piece of
aluminum foil coated in barium platinocyanide
Ba[Pt(CN4)], showed luminescent properties.
• He discovered that placing his hand between the
light source and film resulted in the image of his
skeleton.
• The benefits of x-rays far out weigh the potential
risks
 Inorganic Compounds in Medicine: Examples
In CAT or CT Scans
• Produces more detailed images of internal organs that
traditional x-rays
• Used in diagnosing muscle and bone disorders, locating
blood clots, detecting internal bleeding, monitoring
diseases such as cancer
• To enhance imaging patients are given agents to increase
contrast blocking x-ray transmission
• The Diagnostic agents include:
– Barium Sulphate (BaSO4): oral
– Iodine (I): intravenous
– Barium (Ba)
 Inorganic Compounds in Medicine: Examples

In Magnetic Resonance Imaging (MRI)

Magnetic resonance imaging (MRI) is an imaging technique used
primarily in medical settings to produce high quality images of
the soft tissues of the human body without using x-rays.

It is based on the principles of nuclear magnetic resonance

(NMR) and is a newest and fastest growing field.

How MRI works

A human body is mostly water. Water molecules have hydrogen
nuclei (protons), which become aligned in a magnetic field.

An MRI scanner applies a very strong magnetic which aligns

the proton "spins.“ The scanner also produces a current that creates
a varying magnetic field continued next page
 How MRI works
The protons absorb the energy
from the variable field and flip their
spins. When the field is turned off,
the protons gradually return to
their normal spin.

The return process produces a

radio signal that can be measured
by receivers in the scanner and
made into an image”
 Inorganic Compounds in Medicine: Examples

In Magnetic Resonance Imaging (MRI)

• Inorganic contrast (diagnostic) agents are usually
paramagnetic metal systems which function by altering
hydrogen nuclei of water protons

• Paramagnetic agents are complexes of such as ions Gd,

and Dy. The magnetism of the Gd disrupts the signal from
the water resulting in an improved image. These given by
injection or oral.
• Gd complexes are toxic so chelates are NO
O

used to completely surround the Gd N O O

complex N
Gd
O
OH2

O
N O
O
In Magnetic Resonance Imaging (MRI)
Brain MRI
 Inorganic Compounds in Medicine: Examples
In Technetium (Tc-99m) Imaging
• Technetium pharmaceuticals are metal-electron donor
complexes
• Tc is an electron deficient metal and therefore interacts with
electronegative groups
• Technetium-99m is used as a radioactive tracer and can be
detected in the body by medical equipment (gamma cameras).
Technetium (Tc-99m) Imaging
 Inorganic Compounds in Medicine: Diagnostics
Fluorine
• Fluorine-18 decays to oxygen-18 by
electron capture and then aids imaging by
emitting gamma rays.
• Fluorodeoxyglucose is used in PET Scans
along with Carbon-11, Oxygen-15, and
Nitrogen-13
 Inorganic Compounds in Medicine: Diagnostics
+
OH
OH2
O H2O CO
HO M
HO OH H2O CO
18
F CO
FDG
M = 99mTc, 186Re …64Cu, 68Ga

 FDG is a glucose analogue used for radiotherapy to study

uptake of glucose in the body.

 The inorganic complex on the right is a newer drug in place of

FDG: is inexpensive, more available way to use the powerful
tool of glucose imaging
 Inorganic Medicinal Compounds
a) Therapeutic Agents
 Diagnostic agents are the substances used to examine
the body in order to detect impairment of its normal
functions.

Usually these agents find no other use in medicine.

Diagnostic agents are divided according to the use such as:

• drugs used as radiation contrast media

• drugs used to test organ functions
 Inorganic Medicinal Compounds
Platinum Complexes As Therapeutic Agents

 Cisplatin, carboplatin, oxaliplatin

 Cisplatin interferes with DNA replication, killing the

fastest reproducing cells i.e. cancerous cells. The
interference prompts natural DNA repair.
 Inorganic Medicinal Compounds
Platinum Complexes As Therapeutic Agents

 Cisplatin for treatment of testicular cancer, ovarian cancer,

breast cancer, bladder cancer, cervical cancer, lung cancer,
brain tumors. It is used by injection into a vein.
 The use of cisplatin in testicular cancer has been incredible.
Significant in treatment of ovarian and bladder cancers
observed.
Inorganic Medicinal Compounds
Synthesis of Cisplatin
 Inorganic Medicinal Compounds
Gold Compounds as Antiarthritic Agents
Used in treatment of rheumatoid arthritis

Rheumatoid arthritis primarily affects the membrane that lines

and lubricates a joints

Gold compounds interferes with the process that causes the

joint pain and swelling.
 Inorganic Medicinal Compounds
Chelation Therapry of Heavy Metal Poisoning
• Chelates are chemical Compounds - chemically inactivate
the poison
• Compete with enzyme systems for the metals
• Reverse the metals toxic effects
• Enhance the excretion of the metal
• The chelates formed is a stable compound and water
soluble which are excreted by the kidneys
• An effective chelate should reach parts of the parts of the
body where the heavy metal is
 Inorganic Medicinal Compounds
Chelation Therapry of Metal Poisoning
Examples of Inorganic Chelates
1. calcium disodium EDTA - can cause renal problems, fever, dermatitis (skin
infection).
2. calcium disodium EDTA bind metal ions in the practice of chelation
therapy, e.g., for treating mercury and lead poisoning.
 Inorganic Medicinal Compounds
Chelation Therapry of Metal Poisoning
1. Because of its high binding affinity, the lead ion displaces Ca2+ from its
bond in calcium disodium EDTA .
2. After being bound by the heavy metal ions remain in solution but display
diminished reactivity
3. The lead-containing chelate is eliminated renally-(kidney)
 Inorganic Medicinal Compounds
Boron Neutron Capture Therapy
Radiation therapy: treatment of tumor cells by radiation.
 The process involves:

•the infusion or delivery of a capture compound, which

preferentially concentrates in the tumor,

•then the irradiation of the tumor site by neutrons.

 The isotope B-10 is often used as the neutron capture

agent, in this case NCT is called Boron Neutron Capture
Therapy (BNCT).
 Inorganic Medicinal Compounds
Boron Neutron Capture Therapy
 Advantages of BNCT method:
• a possibility to destroy tumors without highly
traumatic surgical operation

• a possibility to give high radiation doses in

malignant cells that do not destroy healthy ones

Application

• in oncology, especially treating tumors in brain

• veterinary medicine

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