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ANTI-VIRAL DRUGS
Dept. of Medicinal Chemistry
SREE DATTHA INSTITUTE OF PHARMACY,
Sheriguda,Ibrahimpatnam,Telangana-501510
Under the guidance of:
Asst. Professor. Ms. G.Nikitha
Presented by:
CH. Shadgun-16U21R0050
1
SREE DATTHA INSTITUTE OF PHARMACY
INTRODUCTION
• Viruses are ultramicroscopic, obligate, Intracellular
disease causing agents.
• Viruses are inactive in outside the body of host but get
activated with in the host.
• Viruses are completely dependent on host cell for their
replication and utilize the energy by host cells during
protein synthesis and replication of nucleic acid.
2
SREE DATTHA INSTITUTE OF PHARMACY
TYPES OF VIRUSES
• Viruses posses only one type of nucleic acid either DNA
or RNA.
• They contain a protein coat that surrounds nucleic acid.
• The protein coat is known as capsid which is made up of
smaller units.
3
SREE DATTHA INSTITUTE OF PHARMACY
DNA Viruses
VIRUSES INFECTION
Human adenoviruses Upper respiratory tract &
eye infection
Hepatitis-B virus Hepatitis-B
Pox virus Smallpox
Varicella zoster virus chicken pox
4
SREE DATTHA INSTITUTE OF PHARMACY
RNA Viruses
VIRUSES INFECTION
Arena virus Meningitis
Arbovirus Yellow Fever
Influenza virus Influenza
Retro virus AIDS, Leukaemia
Picornavirus Polio, Upper respiratory tract
infections
Rhabdo viruses Rabies
5
SREE DATTHA INSTITUTE OF PHARMACY
Viral Replication
• Adsorption and penetration into susceptible
host cells.
• Un coating of viral nucleic acid.
• Synthesis of early regulatory proteins.
• Synthesis of RNA or DNA.
• Synthesis of late regulatory proteins.
• Assembly(Maturation) of viral particles.
• Release from cells.
6
SREE DATTHA INSTITUTE OF PHARMACY
Mechanism of anti-viral agents
7
SREE DATTHA INSTITUTE OF PHARMACY
Classification
A) Substances that inhibit early stages of viral
replication.
B) Substances that interfere with viral nucleic acid
replication.
C) Substances that affect translation on cell ribosomes.
8
SREE DATTHA INSTITUTE OF PHARMACY
Ideal Properties
• It must posses broad spectrum of antiviral
properties.
• It should completely inhibit viral replication.
• It should have minimum toxicity to host cells
• It should be against resistant viruses.
• It should reach target organ.
9
SREE DATTHA INSTITUTE OF PHARMACY
Acyclovir
• It is an acyclic 2-deoxy guanosine derivative is a pro drug
that gets activated in virus infected cells by
phosphorylation which given by oral, I.V, or topical
routes.
10
SREE DATTHA INSTITUTE OF PHARMACY
Synthesis of Acyclovir
11
SREE DATTHA INSTITUTE OF PHARMACY
Mechanism of Action
• Acyclovir is activated after 3 phosphorylation steps by
viral specific enzymes termed thymidine kinases .
• These active metabolism accumulate in the infected cells
& exert their action by two metabolism.
1) Competitive inhibition of herpes virus DNA
polymerase.
2) Incorporation of Acyclovir into DNA[viral].
12
SREE DATTHA INSTITUTE OF PHARMACY
Uses
• It has been used for the treatment of herpes
virus infections.
• It is used in the treatment of chickenpox, herpes
simplex encephalitis in normal host & varicella
zoster viral infections.
13
SREE DATTHA INSTITUTE OF PHARMACY
Zidovudine
14
SREE DATTHA INSTITUTE OF PHARMACY
Synthesis of Zidovudine
15
SREE DATTHA INSTITUTE OF PHARMACY
Mechanism of Action
• Zidovudine gains access into infected cell by diffusion.
• Once the cell the enzyme thymidine kinase catalysis the
phosphorylation of zidovudine converted into
zidovudine 5-mono-di- & Triphosphate .
• The triphosphate competes with the nucleoside
substrate in the DNA.
• The essential requirement for the formation of 5-3-
phosphodiester bond resulting in the elongation of DNA
chain in presence of oh group at 3rd position of de-oxy
ribose sugar.
16
SREE DATTHA INSTITUTE OF PHARMACY
Uses
• Used in the treatment of HIV-I, HIV-II & human T-cell
lymphotrophic viral infection.
• When administered in both adults & children suffering
from AIDS for prolong life span.
17
SREE DATTHA INSTITUTE OF PHARMACY
18
SREE DATTHA INSTITUTE OF PHARMACY

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Shadgun(anti viral drugs)

  • 1. ANTI-VIRAL DRUGS Dept. of Medicinal Chemistry SREE DATTHA INSTITUTE OF PHARMACY, Sheriguda,Ibrahimpatnam,Telangana-501510 Under the guidance of: Asst. Professor. Ms. G.Nikitha Presented by: CH. Shadgun-16U21R0050 1 SREE DATTHA INSTITUTE OF PHARMACY
  • 2. INTRODUCTION • Viruses are ultramicroscopic, obligate, Intracellular disease causing agents. • Viruses are inactive in outside the body of host but get activated with in the host. • Viruses are completely dependent on host cell for their replication and utilize the energy by host cells during protein synthesis and replication of nucleic acid. 2 SREE DATTHA INSTITUTE OF PHARMACY
  • 3. TYPES OF VIRUSES • Viruses posses only one type of nucleic acid either DNA or RNA. • They contain a protein coat that surrounds nucleic acid. • The protein coat is known as capsid which is made up of smaller units. 3 SREE DATTHA INSTITUTE OF PHARMACY
  • 4. DNA Viruses VIRUSES INFECTION Human adenoviruses Upper respiratory tract & eye infection Hepatitis-B virus Hepatitis-B Pox virus Smallpox Varicella zoster virus chicken pox 4 SREE DATTHA INSTITUTE OF PHARMACY
  • 5. RNA Viruses VIRUSES INFECTION Arena virus Meningitis Arbovirus Yellow Fever Influenza virus Influenza Retro virus AIDS, Leukaemia Picornavirus Polio, Upper respiratory tract infections Rhabdo viruses Rabies 5 SREE DATTHA INSTITUTE OF PHARMACY
  • 6. Viral Replication • Adsorption and penetration into susceptible host cells. • Un coating of viral nucleic acid. • Synthesis of early regulatory proteins. • Synthesis of RNA or DNA. • Synthesis of late regulatory proteins. • Assembly(Maturation) of viral particles. • Release from cells. 6 SREE DATTHA INSTITUTE OF PHARMACY
  • 7. Mechanism of anti-viral agents 7 SREE DATTHA INSTITUTE OF PHARMACY
  • 8. Classification A) Substances that inhibit early stages of viral replication. B) Substances that interfere with viral nucleic acid replication. C) Substances that affect translation on cell ribosomes. 8 SREE DATTHA INSTITUTE OF PHARMACY
  • 9. Ideal Properties • It must posses broad spectrum of antiviral properties. • It should completely inhibit viral replication. • It should have minimum toxicity to host cells • It should be against resistant viruses. • It should reach target organ. 9 SREE DATTHA INSTITUTE OF PHARMACY
  • 10. Acyclovir • It is an acyclic 2-deoxy guanosine derivative is a pro drug that gets activated in virus infected cells by phosphorylation which given by oral, I.V, or topical routes. 10 SREE DATTHA INSTITUTE OF PHARMACY
  • 11. Synthesis of Acyclovir 11 SREE DATTHA INSTITUTE OF PHARMACY
  • 12. Mechanism of Action • Acyclovir is activated after 3 phosphorylation steps by viral specific enzymes termed thymidine kinases . • These active metabolism accumulate in the infected cells & exert their action by two metabolism. 1) Competitive inhibition of herpes virus DNA polymerase. 2) Incorporation of Acyclovir into DNA[viral]. 12 SREE DATTHA INSTITUTE OF PHARMACY
  • 13. Uses • It has been used for the treatment of herpes virus infections. • It is used in the treatment of chickenpox, herpes simplex encephalitis in normal host & varicella zoster viral infections. 13 SREE DATTHA INSTITUTE OF PHARMACY
  • 15. Synthesis of Zidovudine 15 SREE DATTHA INSTITUTE OF PHARMACY
  • 16. Mechanism of Action • Zidovudine gains access into infected cell by diffusion. • Once the cell the enzyme thymidine kinase catalysis the phosphorylation of zidovudine converted into zidovudine 5-mono-di- & Triphosphate . • The triphosphate competes with the nucleoside substrate in the DNA. • The essential requirement for the formation of 5-3- phosphodiester bond resulting in the elongation of DNA chain in presence of oh group at 3rd position of de-oxy ribose sugar. 16 SREE DATTHA INSTITUTE OF PHARMACY
  • 17. Uses • Used in the treatment of HIV-I, HIV-II & human T-cell lymphotrophic viral infection. • When administered in both adults & children suffering from AIDS for prolong life span. 17 SREE DATTHA INSTITUTE OF PHARMACY