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By-
Narayan Prahlad. V
4th
Se m e ste r Mo l. Bio
Guide d By-
Dr. Shaukath Ara Kahnum
De pt. O f Che m istry
Introduction
Classification
Chemotherapeutic Agents
-Antibacterial
-Sulphadrugs
-Antimalarial Agents
-Antipyretics
Important Chemotherapeutic Agents
Chemotherapy
Action of Chemotherapeutic Agents
Conclusion
Reference
Acknowledgement
• Drug is a compound that interacts with the
biological system and triggers a physiological
effect.
Examples: Antibiotic , Antimalarial , Antiviral etc.,
• Drug is derived from a French word “Drogue”
meaning Dry Herb.
Examples: Paracetamol, Penicillin etc.,
According to Therapeutic Agents-
1.Chemotherapeutic Agents
2.Pharmacodynamic Agents
3.Hormones
4.Vitamins
• Treatment of infectious diseases
• Designed to kill invading microbes selectively
without affecting the host.
Examples: Antibacterial, Antiviral, Antifungal
agents etc.,
Pharmacodynamic Agents
• Act on various functions/systems of body like
CNS.
Examples: Tranquilizer, Antidepressants etc.,
• PaulEhlrich-first scientist to use chemicals
against infectious diseases.
• 1904-profounded the principle of chemotherapy-
“Chemicals couldinterferewiththeproliferationof disease
causingmicrobes at theconcentrationleveltoleratedbythe
host.”
• Over the next 20 years efforts were made to create drugs
which would fight disease causing microbes.
• Then there was an important breakthrough when a
Yellow coloured compound-Proflavin(Antibacterial
Agent) was synthesized.
Proflavin
• Used to treat wounds but was ineffective in blood
stream against bacteria.
• In 1935 Prontosilwas created-prodrug for a class
of drugs-Sulphadrugs.
Prontosil
• They are those which fight bacteria.
• Reproduction rate is very high. Some double
every 15 minutes while some every half an hour.
• Some transmit deadly diseases like T.B,
Diphtheria etc.,
• Are chemicals produced by a microbe that is antagonistic
to another microbe at a specific concentration.
Example: Penicillin
• From Pe nicillium and fights against Tre po ne m a pallidium
(Syphilis)
• There are different types of antibiotics-
Beta Lactam-
Penicillin
Tetracyclins:
Consist of a system of four fused six membered
rings.
Examples: Chlorotetracyclin
• First isolated by Duggar in 1947 from
Stre pto m yce s aure o facie ns.
• Used to treat Co njunctivitis in cats.
• Synthetic compounds.
• Since Azodyes bind to animal protein effectively
scientists started to screen azodyes for their
ability to bind to bacterial proteins.
• Also Prontosil was found to have least toxicity.
• Ge rhard Do m ag k applied prontosil for the first
time as a therapeutic agent on his daughter who
was infected with Staphylo co ccus infection.
Soon it was studied-Prontosil was a Prodrug that
got converted to p-acetamidobenzene
sulphonamide within the body.
p-acetamidobenzenesulphonamide
• Later Scientists synthesized this and put it to test. Interestingly it
showed Antibacterial activity.
• Malaria-protozoal disease.
• Protozoan-Plasm o dium vivax, P. m alaria, P. o vale
& P. falciparum .
• Vector- Female Anopheles mosquito.
P. m alaria P. falciparum
P. vivax
P. o vale
• Drug is designed in such a
way-it attacks at various
stages of the malarial cycle.
• Wise to attack it at
sporozoites stage before it
attacks the liver.
Example: 4-aminoquinolines
inhibit the entry of merozoites
into the blood cells of host.
4-Aminoquinoline
• Literally “Against Fire”.
• Drugs used to reduce fever and body
temperature.
• Most common- Aspirin, Ibuprofen etc.,
• Primarily used for relieving pain.
Paracetamol:
Structure-
N-acetyl-p-amino phenol
• Also called Ace tam ino phe n (APAP).
• Widely used to relieve pain and reduce fever.
• Mild analgesic and major ingredient in cold and flu
remedies.
Uses-
• Reduce pain and fever in people.
• In children only if temperature is more than
38.5˚C/101.3˚F
• Better tolerated than aspirin in patients with high
gastric acid secretion and prolonged bleeding.
• Relieve pain in mild arthritis.
Sulpfanilamide:
Structure-
• First prepared by PaulG e lm o 1908.
• It’s a sulphonamide antibacterial.
• Contains a molecule of sulphonamide functional
group attached to aniline.
4-aminobenzene
sulphonamide
Uses-
• Sulphonamide-antibiotic character.
• Inhibits enzyme reactions involving p-
aminobenzoic acid(PABA) which is needed in
enzymatic reactions to produce Folic
acid(coenzyme) which is very much needed for
the synthesis of purines, pyrimidines and amino
acids.
Sulfaguanidine:
Structure-
• It is a sulfadrug containing sulfonamide.
• Used in the treatment of pneumonia, throat
infection etc.,
4-am ino -N[am ino (im ino )m e thyl] be nze ne sulpho nam ide
• Tre atm e nt o f a dise ase by using che m icals which
is adm iniste re d at a particular co nce ntratio n and
at a particular tim e .
• Sidne y Farbe r and PaulEhlrich are regarded as
the father of Modern Chemotherapy.
• Different types of chemotherapeutic agents like
Alkylating Agents, Antimetabolites etc.,
• Some drugs form a coat around the cell and thus
prevent it from any activity.
• Some bind to the receptors and thus block synthesis
of important molecules.
• Few of them interact with the enzyme or group of
enzymes thus inhibiting the synthesis of certain
molecules.
Example: Beta Lactam(Penicillin) blocks the active site
for cell wall synthesis.
• Some drugs act antagonistic to the essential metabolite
of the invading microbe.
Example: Sulphadrug antagonize the essential metabolite
p-am ino be z o ic acid(PABA). The essential structural unit to
all sulphadrugs-p-am ino be nze ne sulpho nam ide unit.
This is very similar to PABA in shape, size, and polarity but
slightly different. So the microbe incorporates p-
aminobenzene sulphonamide due to which many
important molecules cannot ne synthesized.
• Some make pores in the cell which later kill it.
• Drugs are very important chemicals in todays world.
• Without them diseases cannot be fought easily.
• They are the ones that protect our body from microbial attack.
• All the the drugs cannot fight all types of diseases like HIV and
so on as these microbes keep mutating themselves in order to
adapt.
• Lastly it is a better field for researching and finding new drugs
so that we can protect not just man but other creatures too.
• Carey,F.A., and J Sunderberg.2000. Advanced Organic
Chemistrey,4th
Edn.,New York.
• www.elmhurst.edu
• www.ncbi.nlm.nih.gov
• Would like to thank Shaukath Mam for her valuable
guidance.
• Also Dr. N.S. Devaki for providing me this opportunity.
• Thank You All for your patient listening.
Thank You

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Drugs

  • 1. By- Narayan Prahlad. V 4th Se m e ste r Mo l. Bio Guide d By- Dr. Shaukath Ara Kahnum De pt. O f Che m istry
  • 2. Introduction Classification Chemotherapeutic Agents -Antibacterial -Sulphadrugs -Antimalarial Agents -Antipyretics Important Chemotherapeutic Agents Chemotherapy Action of Chemotherapeutic Agents Conclusion Reference Acknowledgement
  • 3. • Drug is a compound that interacts with the biological system and triggers a physiological effect. Examples: Antibiotic , Antimalarial , Antiviral etc., • Drug is derived from a French word “Drogue” meaning Dry Herb. Examples: Paracetamol, Penicillin etc.,
  • 4. According to Therapeutic Agents- 1.Chemotherapeutic Agents 2.Pharmacodynamic Agents 3.Hormones 4.Vitamins
  • 5. • Treatment of infectious diseases • Designed to kill invading microbes selectively without affecting the host. Examples: Antibacterial, Antiviral, Antifungal agents etc., Pharmacodynamic Agents • Act on various functions/systems of body like CNS. Examples: Tranquilizer, Antidepressants etc.,
  • 6. • PaulEhlrich-first scientist to use chemicals against infectious diseases.
  • 7. • 1904-profounded the principle of chemotherapy- “Chemicals couldinterferewiththeproliferationof disease causingmicrobes at theconcentrationleveltoleratedbythe host.” • Over the next 20 years efforts were made to create drugs which would fight disease causing microbes. • Then there was an important breakthrough when a Yellow coloured compound-Proflavin(Antibacterial Agent) was synthesized. Proflavin
  • 8. • Used to treat wounds but was ineffective in blood stream against bacteria. • In 1935 Prontosilwas created-prodrug for a class of drugs-Sulphadrugs. Prontosil
  • 9. • They are those which fight bacteria. • Reproduction rate is very high. Some double every 15 minutes while some every half an hour. • Some transmit deadly diseases like T.B, Diphtheria etc.,
  • 10. • Are chemicals produced by a microbe that is antagonistic to another microbe at a specific concentration. Example: Penicillin • From Pe nicillium and fights against Tre po ne m a pallidium (Syphilis) • There are different types of antibiotics- Beta Lactam- Penicillin
  • 11. Tetracyclins: Consist of a system of four fused six membered rings. Examples: Chlorotetracyclin
  • 12. • First isolated by Duggar in 1947 from Stre pto m yce s aure o facie ns. • Used to treat Co njunctivitis in cats.
  • 13. • Synthetic compounds. • Since Azodyes bind to animal protein effectively scientists started to screen azodyes for their ability to bind to bacterial proteins. • Also Prontosil was found to have least toxicity. • Ge rhard Do m ag k applied prontosil for the first time as a therapeutic agent on his daughter who was infected with Staphylo co ccus infection.
  • 14. Soon it was studied-Prontosil was a Prodrug that got converted to p-acetamidobenzene sulphonamide within the body. p-acetamidobenzenesulphonamide • Later Scientists synthesized this and put it to test. Interestingly it showed Antibacterial activity.
  • 15. • Malaria-protozoal disease. • Protozoan-Plasm o dium vivax, P. m alaria, P. o vale & P. falciparum . • Vector- Female Anopheles mosquito. P. m alaria P. falciparum P. vivax P. o vale
  • 16. • Drug is designed in such a way-it attacks at various stages of the malarial cycle. • Wise to attack it at sporozoites stage before it attacks the liver. Example: 4-aminoquinolines inhibit the entry of merozoites into the blood cells of host. 4-Aminoquinoline
  • 17. • Literally “Against Fire”. • Drugs used to reduce fever and body temperature. • Most common- Aspirin, Ibuprofen etc., • Primarily used for relieving pain.
  • 19. • Also called Ace tam ino phe n (APAP). • Widely used to relieve pain and reduce fever. • Mild analgesic and major ingredient in cold and flu remedies. Uses- • Reduce pain and fever in people. • In children only if temperature is more than 38.5˚C/101.3˚F
  • 20. • Better tolerated than aspirin in patients with high gastric acid secretion and prolonged bleeding. • Relieve pain in mild arthritis.
  • 21. Sulpfanilamide: Structure- • First prepared by PaulG e lm o 1908. • It’s a sulphonamide antibacterial. • Contains a molecule of sulphonamide functional group attached to aniline. 4-aminobenzene sulphonamide
  • 22. Uses- • Sulphonamide-antibiotic character. • Inhibits enzyme reactions involving p- aminobenzoic acid(PABA) which is needed in enzymatic reactions to produce Folic acid(coenzyme) which is very much needed for the synthesis of purines, pyrimidines and amino acids.
  • 23. Sulfaguanidine: Structure- • It is a sulfadrug containing sulfonamide. • Used in the treatment of pneumonia, throat infection etc., 4-am ino -N[am ino (im ino )m e thyl] be nze ne sulpho nam ide
  • 24. • Tre atm e nt o f a dise ase by using che m icals which is adm iniste re d at a particular co nce ntratio n and at a particular tim e . • Sidne y Farbe r and PaulEhlrich are regarded as the father of Modern Chemotherapy. • Different types of chemotherapeutic agents like Alkylating Agents, Antimetabolites etc.,
  • 25. • Some drugs form a coat around the cell and thus prevent it from any activity. • Some bind to the receptors and thus block synthesis of important molecules. • Few of them interact with the enzyme or group of enzymes thus inhibiting the synthesis of certain molecules. Example: Beta Lactam(Penicillin) blocks the active site for cell wall synthesis.
  • 26. • Some drugs act antagonistic to the essential metabolite of the invading microbe. Example: Sulphadrug antagonize the essential metabolite p-am ino be z o ic acid(PABA). The essential structural unit to all sulphadrugs-p-am ino be nze ne sulpho nam ide unit. This is very similar to PABA in shape, size, and polarity but slightly different. So the microbe incorporates p- aminobenzene sulphonamide due to which many important molecules cannot ne synthesized. • Some make pores in the cell which later kill it.
  • 27. • Drugs are very important chemicals in todays world. • Without them diseases cannot be fought easily. • They are the ones that protect our body from microbial attack. • All the the drugs cannot fight all types of diseases like HIV and so on as these microbes keep mutating themselves in order to adapt. • Lastly it is a better field for researching and finding new drugs so that we can protect not just man but other creatures too.
  • 28. • Carey,F.A., and J Sunderberg.2000. Advanced Organic Chemistrey,4th Edn.,New York. • www.elmhurst.edu • www.ncbi.nlm.nih.gov
  • 29. • Would like to thank Shaukath Mam for her valuable guidance. • Also Dr. N.S. Devaki for providing me this opportunity. • Thank You All for your patient listening.