SlideShare a Scribd company logo
1 of 45
Download to read offline
ANTI-VIRAL DRUGS
Lecture 1
Medicinal Chemistry IV
Dr.Narmin Hama Amin
University of Sulaimani
College of Pharmacy
Anti-Viral Drugs
▪ Antiviral agents are substances used in the treatment and prophylaxis
of diseases caused by viruses.
▪ Viral diseases include influenza, rabies, yellow fever, poliomyelitis,
ornithosis, mumps, measles, ebola, human immuno deficiency virus
(HIV), herpes, warts, and small pox
What are Viruses?
▪ Viruses are the smallest infectious agents that replicates only inside
the living cells of other organisms.
▪ Viruses cannot reproduce on their Own , they use host’s metabolic
processes
▪ Range in size from about 20 nm to about 300 nm in diameter
▪ Viruses are lack both a cell wall and cell membrane and they do not
carry out metabolic process
Comparison between viruses and bacteria
Structure Of Viruses
➢ The complete structure is known as a virion
▪ Viral particles consist of two to three parts
1. Genetic material , either DNA or RNA
2. Protein coat (Capsid), which surrounds and protects the genetic material
3. Envelope of lipid , lipid layer that surround the protein coat when they are outside cell
Classification of Viruses:
▪Herpes viruses to combat diseases such as cold sores, genital herpes
▪ Chicken pox & Shingles
▪ Eye diseases
▪Papillomavirus
▪Hepatitis B virus
▪Mononucleosis
RNA viruses:
▪ HIV ( Human immuno deficiency virus)
▪ AIDS ( Acquired immune deficiency syndrome)
▪Hepatitis C
▪ Influenza (or flu) is an airborne, respiratory disease caused by an RNA virus
▪Cold virus
▪Coronavirus
DNA Viruses
Examples of viruses with diseases
Life cycle of the viruses
➢
Examples of viral receptors
Life cycle of influenza
Herpes simplex virus(HSV) structure
▪Herpes simplex viruses -- more commonly
known as herpes are categorized into two types:
A. Herpes type 1 (HSV-1, or oral herpes)
B. Herpes type 2 (HSV-2, or genital herpes)
RNA virus (HIV) life cycle
▪ HIV can lead to the
development of AIDS. AIDS, or
stage 3 HIV, develops when
HIV has caused serious
damage to the immune system
▪ Diagram of hepatitis B virus (HBV) replication cycle. Attachment to the
sodium taurocholate co-transporting polypeptide (NTCP) receptor, and
possibly other receptors too, is the initiating event of The sodium
taurocholate co-transporting polypeptide (NTCP), a transmembrane protein
highly expressed in human hepatocytes that mediates the transport of bile
acids, plays a key role in HBV and HDV entry into hepatocytes.
▪ Recently, NTCP has been shown to modulate HCV infection of hepatocytes
by regulating innate antiviral immune responses in the liver.
▪ AN EPIDEMIC is a disease that affects a large number of people within a community,
population, or region.
▪ A PANDEMIC is an epidemic that’s spread over multiple countries or continents.
➢ For example, when COVID-19 was limited to Wuhan, China, it was an epidemic. The
geographical spread turned it into a pandemic.
▪ ENDEMIC is something that belongs to a particular people or country.
▪ AN OUTBREAK is a greater-than-anticipated increase in the number of endemic cases.
It can also be a single case in a new area. If it’s not quickly controlled, an outbreak can
become an epidemic
The major sites for anti-viral drugs
Classification of Anti-viral Drugs:
1. Viral attachment and entry are blocked by:
A. Maraviroc(HIV) :
▪It is new class of antiretroviral agents , approved as a chemokine receptor CCR5
antagonist in 2007 and is the first anti-HIV agent to act on a molecular target on
the host cell rather than the virus
▪Block human immunodeficiency virus type 1 (HIV-1) attachment to the coreceptor
and prevents the virus from entering CD4+ cells.
▪It is an example of an agent that works by blocking protein–protein interactions
between a viral protein and a host cell protein
▪Maraviroc is a substrate of cytochrome P450 (CYP3A) and p-glycoprotein, and
has clinically significant interactions with other drugs including efavirenz and
rifampin.
B. Enfuvirtide(Fuzeon):
▪Enfuvirtide (INN) is an HIV fusion inhibitor, the first of a class of antiretroviral
drugs used in combination therapy for the treatment of HIV-1 infection
▪Exhibits potent and selective inhibition of membrane of viral and cells.
▪ It is a linear 36-amino acid synthetic peptide with the N-terminus acetylated and
the C-terminus is a carboxamide. It is composed of naturally occurring L-amino
acid residues.
2- Penetration Inhibitors
▪ Interferon α-2B
▪Interferon-mediated inhibition of virus penetration.
▪Interferon is a powerful drug used to treat hepatitis types B, C, and D. It can
prevent serious liver damage. It also finds its usefulness in lung carcinoma,
breast cancer, multiple myclomas. It is also recommended as a prophylactic
agent in cytomegalovirus infection
▪Interferons are proteins that are secreted by the cells when the body is
being attacked by a virus like hepatitis B, C, or D. Genetically engineered
interferon, given by injection, stops the hepatitis virus from replicating itself
and provides a boost to the immune system.
▪ In general, interferons are made up of a mixture of relatively small proteins
with molecular weights varying from 20,000 to 1,60,000. These are basically
glycoproteins that display specific antiviral properties with species-related
characteristics.
Pegylated interferon:
▪Pegylated interferon, usually called peginterferon, is a chemically modified form
of the standard interferon that treats hepatitis C and rarely hepatitis B.
▪It is also used with ribavirin against hepatitis C infections.
▪The difference between interferon and peginterferon is the PEG, which stands for
a molecule called polyethylene glycol.
▪The PEG does nothing to fight the virus, in these formulations, Polyethylene
glycol (PEG) is added to make interferon last longer in the body
▪Pegylated interferon is contraindicated in patients with hyperbilirubinaemia.
Ribavirin, also known as tribavirin, is an antiviral medication used to
treat RSV infection, hepatitis C and some viral hemorrhagic fevers.
For hepatitis C, it is used in combination with other medications such as
simeprevir, sofosbuvir, peginterferon alfa-2b or peginterferon alfa-2a.
Producing a broad-spectrum activity against several RNA and DNA
viruses, Ribavirin is a synthetic guanosine nucleoside and antiviral agent
that interferes with the synthesis of viral mRNA.
3- Uncoating Inhibitors:
Adamantane amines group
▪ They are hydrophobic amines (weak organic bases) with clinical against influenza
A ( amantadine and rimantadine) .
▪ Their specificity stems from their ability to bind to block the proton channel formed
by the M2 matix protein. The M2 proton channel of the Influenza A virus is the
target of the anti-influenza drugs amantadine and rimantadine
▪ Can reduce severity of illness if started within 48 hrs of onset of symptoms.
➢Rimantadine:
▪ Its methyl derivative of amantadine .
▪Interfere with virus uncoating by inhibiting release of specific
protein also its more effective and less toxic than amantadine
Synthesis of Rimantadine:
1-adamantyl methyl ketoxime
1- acetyladamantane
Amantadine , inhibit the uncoating of the viral RNA within the
infected host cells thus preventing its replication.
▪ Amantadine is used in the treatment of Parkinson’s disease. It is
effective against influenza type-A virus, para influenza, and some
RNA virus. It is also used as a dopamine receptor agonist.
Synthesis of Amantadine
➢ Tromantadine:
▪ Tromantadine is an antiviral medicine used to treat herpes
simplex virus. It is available in a topical gel under trade
names Viru-Merz and Viru-Merz Serol. Its performance is
similar to acyclovi.
▪ Tromantadine inhibits the early and late events in the virus
replication cycle. It changes the glycoproteins of the host
cells, therefore impeding the absorption of the virus. It
inhibits penetration of the virus. It also prevents uncoating of
the virions.
Synthesis of Tromantadine
(amantadine)
3- Protease inhibitors:
▪Protease inhibitors (PIs) are a class of antiviral drugs
that are widely used to treat HIV/AIDS and hepatitis
caused by hepatitis C virus.
▪Protease inhibitors prevent viral replication by
selectively binding to viral proteases (e.g. HIV-1
protease) and blocking proteolytic cleavage of protein
precursors that are necessary for the production of
infectious viral particles.
▪HIV-1 protease is a retroviral aspartyl protease, an
enzyme involved with peptide bond hydrolysis in
retroviruses, that is essential for the life-cycle of HIV, the
retrovirus that causes AIDS.
A- Saquinavir: was developed by Roche and, as the first PI to reach the market.
It has large molecular weight and peptide-like character.
▪It is used to treat HIV infections
▪ It is approximately 98% bound to plasma proteins.
▪Poor oral bioavailability, but is increased with a fatty meal.
▪The drug should be used in combination with at least two
other antiretroviral drugs to minimize resistance.
B-Indinavir: has better oral bioavailability than saquinavir and is less highly bound
to plasma proteins (60%).
▪ When administered with a high-fat diet, indinavir achieves a maximum serum
concentration of 77% of the administered dose.
C- Nelfinavir: was marketed in 1997 and is used as part of a four-drug
combination therapy. Like indinavir and ritonavir, nelfinavir is more potent than
saquinavir because of its better pharmacokinetic profile.
▪ Compared with saquinavir, it has a lower molecular
weight and log P , and an enhanced aqueous solubility
, resulting in enhanced oral bioavailability.
D- Atazanavir was approved in June 2003 as the first
once daily HIV-1 PI to be used as part of a combination
therapy. It is usually administered with ritonavir.
E- Lopinavir is a protease inhibitor that has been approved for use in
combination with ritonavir for patients with HIV who have not responded to other
treatment modalities.
▪ Ritonavir inhibits lopinavir’s metabolism by
CYP3A4, causing a higher level of lopinavir
in the system.
F- Tipranavir. is unique among the PIs because it is not a peptidomimetic
compound. It does appear to bind to the active site of HIV-1 protease the
same as the peptidomimetics do.
▪ The benefit of this agent is that, because it is a different chemical structure,
cross-resistance does not develop to the same extent as seen with the
peptidomimetics.
▪ It is used to treat HIV infections that are resistant to other PIs. However,
there have been cases of life-threatening liver toxicity
▪ The drug is administered with a booster dose of ritonavir. This protocol
inhibits CYP3A4, causing the levels of tipranavir to increase..
G - Ritonavir: is an antiretroviral medication used along with other medications to
treat HIV/AIDS. This combination treatment is known as highly active antiretroviral
therapy (HAART).Often a low dose is used with other protease inhibitors.
• It may also be used in combination with other medications for hepatitis C.It is
taken by mouth.
• Ritonavir ,amprenavir and nelfinavir have similar properties and cautionary
statements. All cause dyslipidemia, and they have a host of drug interactions,
mainly because they inhibit CYP3A4. These agents must always be used with at
least two other antiretroviral agents. Used properly, the PIs are an important part
of HIV therapy.
4- Nucleic acid Inhibitors:
▪ These drugs usually act by inhibiting:
A. Polymerases
B. Reverse Transcriptase
▪They are usually analogues of the purine and pyrimidine bases found in
the nucleic acids
Purine nucleotides:-
a) Acyclovir
b) Valacyclovir
c) Gancyclovir
d) Pencyclovir
e) famcyclovir
A- Inhibitors of viral DNA polymerase
A- Acyclovir
▪ It is a drug of choice in both prophylaxis and treatment of
herpes simplex virus, particularly and varicella-zoster(i.e.
chickenpox and shingles) significantly.
▪ Herpetic keratitis and herpes genitals are treated
effectively by using an ointment containing 5%acyclovir.
▪ Acyclovir has a nucleoside-like structure and contains the
same nucleic acid base as deoxyguanosine. However, it
lacks the complete sugar ring.
▪ The oral bioavailability of acyclovir is quite low
SARs Of Acyclovir
1. Acyclovir is an oxopurine that is guanine substituted by a (2-
hydroxyethoxy)methyl substituent at position 9.
2.The length of acyclic side chain attached at N-9 is essential for the anti viral
activity.
3.When the acyclic side chain containing hydroxy methylene group was replaced
by other substituents,inactive analogues are obtained.This implies that –CH2OH
group is essential for anti viral activity.
4.The 9-alkoxy derivative was obtained when a slight modification was brought in
the acyl side chain which is highly active against herpes simplex and varicella
zoster viruses.
5.Several structural modifications have been brought to acyclovir to obtain high
potent drugs.
2-amino-9-(2-hydroxyethoxymethyl)-1H-purin-6-one
Acyclovir
The effect of acyclovir is the inhibition of viral DNA synthesis. Transport into the cell
and monophosphorylation are accomplished by a thymidine kinase that is encoded
by the virus itself. The affinity of acyclovir for the viral thymidine kinase is about 200
times that of the corresponding mammalian enzyme.In virally infected cells, it is
phosphorylated to form a triphosphate which is the active agent, and so acyclovir is
a prodrug .
Acyclovir triphosphate prevents DNA replication in two ways:
Firstly, it can bind to DNA polymerase and inhibit it.
Secondly, the drug acts as a chain terminator
Synthesis of acyclovir
▪ The oral bioavailability of acyclovir is quite low (15– 30%). To overcome this,
various prodrugs were developed to increase water solubility.
B- Valacyclovir is an l-valyl ester prodrug absorbed from the gut far more
effectively than acyclovir.
It is a prodrug intended to increase the bioavailability of acyclovir by increasing
lipophilicity. The oral bioavailability of valacyclovir is three to five times that of
acyclovir
Pencyclovir and its prodrug famciclovir are analogues of ganciclovir.
▪ The clinical usefulness of ganciclovir is limited by the toxicity of the drug.
Ganciclovir causes myelosuppression, producing neutropenia,
thrombocytopenia, and anemia.
In famcyclovir, the two alcohol groups of penciclovir are masked as esters
making the structure less polar, resulting in better absorption.
B- Nucleoside reverse transcriptase inhibitors(NRT I) :
▪ As the enzyme reverse transcriptase is unique to HIV, it serves as an ideal drug
target
➢ Zidovudine was developed originally as an anticancer agent but was the first
drug to be approved for use in the treatment of AIDS.
It is an analogue of deoxythymidine where the sugar
3′-hydroxyl group has been replaced by an azido group
➢lamivudine and emtricitabine: analogues of
deoxycytidine where the 3′ carbon has been replaced
by sulphur.
C-Non-nucleoside reverse transcriptase inhibitors( NNRTI)
➢Nevirapine has a rigid butterfly-like conformation that makes it chiral.
▪ One ‘wing’ interacts through hydrophobic and van der Waals interactions with
aromatic residues in the binding site, while the other wing interacts with
aliphatic residues.
▪ It is used to treat adults and children with human immunodeficiency virus (HIV)
infection.
▪ Nevirapine is more than 90% absorbed by the oral route and is widely
distributed throughout the body. It distributes well into breast milk and crosses
the placenta
5- Release Inhibitors :
Neuraminidase Inhibitors
➢Oseltamivir(Tamiflu)
➢Zanamivir
▪ Drugs use to prevents the Neuraminidase proteins on the surface of IV
removing sialic acid from sialic aid-contanining receptors .
▪ Viral budding and downstream replication of IV are inhibited when sialic acid
remains on the virion membrane and host cell.
Types of influenza or Flu Virus :
▪Type A flu or influenza A viruses are capable of infecting animals, although it is
more common for people to suffer the ailments associated with this type of flu.
Wild birds commonly act as the hosts for this flu virus.
▪Influenza type B viruses are not classified by subtype and do not cause
pandemics.
▪1918 with the death of at least 20 million people worldwide caused by the
Spanish flu virus. Epidemics then occurred in 1957 (Asian flu), 1968 (Hong Kong
flu), and 1977 (Russian flu).
➢Oseltamivir(Tamiflu) first orally active neuraminidase (NA) inhibitor.a
prodrug compound.
➢Active against the influenza A pandemic (H1N1)
➢ Hydrolysis of the ester takes place in the body to give the active carboxylic acid
derivative of oseltamivir.
➢As a structural analogue of a key intermediate in sialic acid/NA chemistry,
oseltamivir serves as a competitive inhibitor of viral NA by binding strongly to the
active site of NA.
➢This interaction ultimately prevents the release of new viral particles from the
host cell.
➢Zanamivir
▪ Effective for both influenza A and B.
▪ Poor bioavailability and poor plasma portion binding
▪Use oral inhalation 4-guanidino-2,4-dideoxy-2,3-dehydro-N- acetyl neuraminic
aid
Anti-Viral Drugs/Medicinal Chemistry

More Related Content

What's hot

Antiviral agents
Antiviral agentsAntiviral agents
Antiviral agentsGanesh Mote
 
Medicinal chemistry- antimalerial agents
Medicinal chemistry- antimalerial agentsMedicinal chemistry- antimalerial agents
Medicinal chemistry- antimalerial agentsDHARMENDRA BARIA
 
Anti viral drugs of medicinal chemistry
Anti viral drugs of medicinal chemistryAnti viral drugs of medicinal chemistry
Anti viral drugs of medicinal chemistryPranjal Saxena
 
Medicinal Chemistry of Antifungal Agents.ppt
Medicinal Chemistry of Antifungal Agents.pptMedicinal Chemistry of Antifungal Agents.ppt
Medicinal Chemistry of Antifungal Agents.pptSalarBasheer
 
Antiviral agents
Antiviral agentsAntiviral agents
Antiviral agentsVedant Bhor
 
ANTI-MALARIAL DRUGS AND ANALOGUES
ANTI-MALARIAL DRUGS AND ANALOGUESANTI-MALARIAL DRUGS AND ANALOGUES
ANTI-MALARIAL DRUGS AND ANALOGUESShikha Popali
 
Antitubercular agents
Antitubercular agentsAntitubercular agents
Antitubercular agentskencha swathi
 
Quinolone antibacterials
Quinolone antibacterialsQuinolone antibacterials
Quinolone antibacterialsSuvarta Maru
 
Important Synthesis of Antiviral Drugs
Important Synthesis of  Antiviral DrugsImportant Synthesis of  Antiviral Drugs
Important Synthesis of Antiviral DrugsAnjali Bhardwaj
 
Antimalarial drugs
Antimalarial drugsAntimalarial drugs
Antimalarial drugsAsra Hameed
 
fluoroquinolones medchem- oriental college of pharmacy
fluoroquinolones medchem- oriental college of pharmacyfluoroquinolones medchem- oriental college of pharmacy
fluoroquinolones medchem- oriental college of pharmacyKaushik Kuche
 
Medicinal chemistry of Antifungal agents
Medicinal chemistry of Antifungal agentsMedicinal chemistry of Antifungal agents
Medicinal chemistry of Antifungal agentsGanesh Mote
 

What's hot (20)

Antiviral agents
Antiviral agentsAntiviral agents
Antiviral agents
 
Medicinal chemistry- antimalerial agents
Medicinal chemistry- antimalerial agentsMedicinal chemistry- antimalerial agents
Medicinal chemistry- antimalerial agents
 
Anti viral drugs of medicinal chemistry
Anti viral drugs of medicinal chemistryAnti viral drugs of medicinal chemistry
Anti viral drugs of medicinal chemistry
 
Medicinal Chemistry of Antifungal Agents.ppt
Medicinal Chemistry of Antifungal Agents.pptMedicinal Chemistry of Antifungal Agents.ppt
Medicinal Chemistry of Antifungal Agents.ppt
 
Anti viral
Anti viralAnti viral
Anti viral
 
AntiViral drug
AntiViral drugAntiViral drug
AntiViral drug
 
Antiviral agents
Antiviral agentsAntiviral agents
Antiviral agents
 
ANTI-MALARIAL DRUGS AND ANALOGUES
ANTI-MALARIAL DRUGS AND ANALOGUESANTI-MALARIAL DRUGS AND ANALOGUES
ANTI-MALARIAL DRUGS AND ANALOGUES
 
Antitubercular agents
Antitubercular agentsAntitubercular agents
Antitubercular agents
 
Med.chem sulfonamides
Med.chem  sulfonamidesMed.chem  sulfonamides
Med.chem sulfonamides
 
Macroloid antibiotics
Macroloid antibioticsMacroloid antibiotics
Macroloid antibiotics
 
Antiviral agents-1
Antiviral agents-1Antiviral agents-1
Antiviral agents-1
 
Antiviral drugs
Antiviral drugsAntiviral drugs
Antiviral drugs
 
Quinolone antibacterials
Quinolone antibacterialsQuinolone antibacterials
Quinolone antibacterials
 
Antiviral drugs
Antiviral drugsAntiviral drugs
Antiviral drugs
 
Antiviral drugs
Antiviral drugsAntiviral drugs
Antiviral drugs
 
Important Synthesis of Antiviral Drugs
Important Synthesis of  Antiviral DrugsImportant Synthesis of  Antiviral Drugs
Important Synthesis of Antiviral Drugs
 
Antimalarial drugs
Antimalarial drugsAntimalarial drugs
Antimalarial drugs
 
fluoroquinolones medchem- oriental college of pharmacy
fluoroquinolones medchem- oriental college of pharmacyfluoroquinolones medchem- oriental college of pharmacy
fluoroquinolones medchem- oriental college of pharmacy
 
Medicinal chemistry of Antifungal agents
Medicinal chemistry of Antifungal agentsMedicinal chemistry of Antifungal agents
Medicinal chemistry of Antifungal agents
 

Similar to Anti-Viral Drugs/Medicinal Chemistry

Antiviral Agents(R1).pptx
Antiviral Agents(R1).pptxAntiviral Agents(R1).pptx
Antiviral Agents(R1).pptxMunFeiYam1
 
Antiviral HIV ARVS AIDS RETROVIRAL
Antiviral HIV ARVS AIDS RETROVIRALAntiviral HIV ARVS AIDS RETROVIRAL
Antiviral HIV ARVS AIDS RETROVIRALLarry Mweetwa
 
Pharmacology of antiretrovirals
Pharmacology      of  antiretroviralsPharmacology      of  antiretrovirals
Pharmacology of antiretroviralsDhananjay Desai
 
Anti viral agents ppt
Anti viral agents pptAnti viral agents ppt
Anti viral agents pptNavdha Soni
 
Antiviral drugs
Antiviral drugsAntiviral drugs
Antiviral drugsCCRMHZN
 
SlideShare On Chemotherapy of Antiviral Drugs (Pharmacology)
SlideShare On Chemotherapy of Antiviral Drugs (Pharmacology)SlideShare On Chemotherapy of Antiviral Drugs (Pharmacology)
SlideShare On Chemotherapy of Antiviral Drugs (Pharmacology)Naveen K L
 
A Presentation on Virus and Anti-Viral Therapy
A Presentation on Virus and Anti-Viral TherapyA Presentation on Virus and Anti-Viral Therapy
A Presentation on Virus and Anti-Viral TherapyGagandeep Jaiswal
 
anti- retroviral drugs.pptx
anti- retroviral drugs.pptxanti- retroviral drugs.pptx
anti- retroviral drugs.pptxMONIKA325654
 
(Nica) anti viral
(Nica) anti viral(Nica) anti viral
(Nica) anti viralNica Teo
 

Similar to Anti-Viral Drugs/Medicinal Chemistry (20)

Antiviral Agents(R1).pptx
Antiviral Agents(R1).pptxAntiviral Agents(R1).pptx
Antiviral Agents(R1).pptx
 
AIDS
AIDSAIDS
AIDS
 
Antiviral HIV ARVS AIDS RETROVIRAL
Antiviral HIV ARVS AIDS RETROVIRALAntiviral HIV ARVS AIDS RETROVIRAL
Antiviral HIV ARVS AIDS RETROVIRAL
 
Pharmacology of antiretrovirals
Pharmacology      of  antiretroviralsPharmacology      of  antiretrovirals
Pharmacology of antiretrovirals
 
Antiviral drugs
Antiviral drugsAntiviral drugs
Antiviral drugs
 
Anti viral drugs
Anti viral drugsAnti viral drugs
Anti viral drugs
 
Anti viral agents ppt
Anti viral agents pptAnti viral agents ppt
Anti viral agents ppt
 
Aids
AidsAids
Aids
 
Anti viral drugs
Anti viral drugsAnti viral drugs
Anti viral drugs
 
Antiviral drugs
Antiviral drugsAntiviral drugs
Antiviral drugs
 
SlideShare On Chemotherapy of Antiviral Drugs (Pharmacology)
SlideShare On Chemotherapy of Antiviral Drugs (Pharmacology)SlideShare On Chemotherapy of Antiviral Drugs (Pharmacology)
SlideShare On Chemotherapy of Antiviral Drugs (Pharmacology)
 
ANTIVIRAL DRUGS (HIV)
ANTIVIRAL DRUGS (HIV)ANTIVIRAL DRUGS (HIV)
ANTIVIRAL DRUGS (HIV)
 
A Presentation on Virus and Anti-Viral Therapy
A Presentation on Virus and Anti-Viral TherapyA Presentation on Virus and Anti-Viral Therapy
A Presentation on Virus and Anti-Viral Therapy
 
anti- retroviral drugs.pptx
anti- retroviral drugs.pptxanti- retroviral drugs.pptx
anti- retroviral drugs.pptx
 
Antiviral Drugs
Antiviral DrugsAntiviral Drugs
Antiviral Drugs
 
Antiviral Drugs
Antiviral DrugsAntiviral Drugs
Antiviral Drugs
 
(Nica) anti viral
(Nica) anti viral(Nica) anti viral
(Nica) anti viral
 
Chemotherapy of hiv
Chemotherapy of hivChemotherapy of hiv
Chemotherapy of hiv
 
aids drugs.pptx
aids drugs.pptxaids drugs.pptx
aids drugs.pptx
 
antiviral drugs
antiviral drugsantiviral drugs
antiviral drugs
 

More from NarminHamaaminHussen

Alkylating agents -Medicinal Chemistry
Alkylating agents -Medicinal Chemistry Alkylating agents -Medicinal Chemistry
Alkylating agents -Medicinal Chemistry NarminHamaaminHussen
 
Antiparasitic drugs-Medicinal Chemistry
Antiparasitic drugs-Medicinal ChemistryAntiparasitic drugs-Medicinal Chemistry
Antiparasitic drugs-Medicinal ChemistryNarminHamaaminHussen
 
Antimalarial agents-Medicinal Chemistry
Antimalarial agents-Medicinal ChemistryAntimalarial agents-Medicinal Chemistry
Antimalarial agents-Medicinal ChemistryNarminHamaaminHussen
 
Antifungal agents-Medicinal Chemistry
Antifungal agents-Medicinal Chemistry Antifungal agents-Medicinal Chemistry
Antifungal agents-Medicinal Chemistry NarminHamaaminHussen
 
Anti-Cancer Drugs-Alkylating agents
Anti-Cancer Drugs-Alkylating agents  Anti-Cancer Drugs-Alkylating agents
Anti-Cancer Drugs-Alkylating agents NarminHamaaminHussen
 
Anti-Cancer Drugs-Medicinal Chemistry
Anti-Cancer Drugs-Medicinal ChemistryAnti-Cancer Drugs-Medicinal Chemistry
Anti-Cancer Drugs-Medicinal ChemistryNarminHamaaminHussen
 
Anthelmintic Drugs-Medicinal Chemistry
Anthelmintic Drugs-Medicinal ChemistryAnthelmintic Drugs-Medicinal Chemistry
Anthelmintic Drugs-Medicinal ChemistryNarminHamaaminHussen
 
Anti -Parkinsonian Drugs-Medicinal Chemistry
Anti -Parkinsonian Drugs-Medicinal ChemistryAnti -Parkinsonian Drugs-Medicinal Chemistry
Anti -Parkinsonian Drugs-Medicinal ChemistryNarminHamaaminHussen
 
Benzodiazepines--Medicinal Chemistry
Benzodiazepines--Medicinal ChemistryBenzodiazepines--Medicinal Chemistry
Benzodiazepines--Medicinal ChemistryNarminHamaaminHussen
 
Antibiotic -Drugs/ Medicinal Chemistry
Antibiotic -Drugs/ Medicinal ChemistryAntibiotic -Drugs/ Medicinal Chemistry
Antibiotic -Drugs/ Medicinal ChemistryNarminHamaaminHussen
 
Antiepileptic drugs / Medicinal Chemistry III
Antiepileptic drugs / Medicinal Chemistry IIIAntiepileptic drugs / Medicinal Chemistry III
Antiepileptic drugs / Medicinal Chemistry IIINarminHamaaminHussen
 
Antipsychotic Drugs/Medicinal Chemistry
Antipsychotic Drugs/Medicinal ChemistryAntipsychotic Drugs/Medicinal Chemistry
Antipsychotic Drugs/Medicinal ChemistryNarminHamaaminHussen
 
Sedative hypnotic drugs /Medicinal Chemistry III(Part Two)
Sedative  hypnotic drugs /Medicinal Chemistry III(Part Two)Sedative  hypnotic drugs /Medicinal Chemistry III(Part Two)
Sedative hypnotic drugs /Medicinal Chemistry III(Part Two)NarminHamaaminHussen
 
Sedative and hypnotic Drugs/ Medicinal Chemistry III (Part One)
Sedative and hypnotic Drugs/  Medicinal Chemistry III (Part One)Sedative and hypnotic Drugs/  Medicinal Chemistry III (Part One)
Sedative and hypnotic Drugs/ Medicinal Chemistry III (Part One)NarminHamaaminHussen
 
local anesthetics / Medicinal Chemistry
local anesthetics / Medicinal Chemistry local anesthetics / Medicinal Chemistry
local anesthetics / Medicinal Chemistry NarminHamaaminHussen
 
General anesthetics / Medicinal Chemistry III
General anesthetics / Medicinal Chemistry IIIGeneral anesthetics / Medicinal Chemistry III
General anesthetics / Medicinal Chemistry IIINarminHamaaminHussen
 

More from NarminHamaaminHussen (17)

Alkylating agents -Medicinal Chemistry
Alkylating agents -Medicinal Chemistry Alkylating agents -Medicinal Chemistry
Alkylating agents -Medicinal Chemistry
 
Antiparasitic drugs-Medicinal Chemistry
Antiparasitic drugs-Medicinal ChemistryAntiparasitic drugs-Medicinal Chemistry
Antiparasitic drugs-Medicinal Chemistry
 
Antimalarial agents-Medicinal Chemistry
Antimalarial agents-Medicinal ChemistryAntimalarial agents-Medicinal Chemistry
Antimalarial agents-Medicinal Chemistry
 
Antifungal agents-Medicinal Chemistry
Antifungal agents-Medicinal Chemistry Antifungal agents-Medicinal Chemistry
Antifungal agents-Medicinal Chemistry
 
Anti-Cancer Drugs-Alkylating agents
Anti-Cancer Drugs-Alkylating agents  Anti-Cancer Drugs-Alkylating agents
Anti-Cancer Drugs-Alkylating agents
 
Anti-Cancer Drugs-Medicinal Chemistry
Anti-Cancer Drugs-Medicinal ChemistryAnti-Cancer Drugs-Medicinal Chemistry
Anti-Cancer Drugs-Medicinal Chemistry
 
Anthelmintic Drugs-Medicinal Chemistry
Anthelmintic Drugs-Medicinal ChemistryAnthelmintic Drugs-Medicinal Chemistry
Anthelmintic Drugs-Medicinal Chemistry
 
Anti -Parkinsonian Drugs-Medicinal Chemistry
Anti -Parkinsonian Drugs-Medicinal ChemistryAnti -Parkinsonian Drugs-Medicinal Chemistry
Anti -Parkinsonian Drugs-Medicinal Chemistry
 
Barbiturates -Medicinal Chemistry
Barbiturates -Medicinal ChemistryBarbiturates -Medicinal Chemistry
Barbiturates -Medicinal Chemistry
 
Benzodiazepines--Medicinal Chemistry
Benzodiazepines--Medicinal ChemistryBenzodiazepines--Medicinal Chemistry
Benzodiazepines--Medicinal Chemistry
 
Antibiotic -Drugs/ Medicinal Chemistry
Antibiotic -Drugs/ Medicinal ChemistryAntibiotic -Drugs/ Medicinal Chemistry
Antibiotic -Drugs/ Medicinal Chemistry
 
Antiepileptic drugs / Medicinal Chemistry III
Antiepileptic drugs / Medicinal Chemistry IIIAntiepileptic drugs / Medicinal Chemistry III
Antiepileptic drugs / Medicinal Chemistry III
 
Antipsychotic Drugs/Medicinal Chemistry
Antipsychotic Drugs/Medicinal ChemistryAntipsychotic Drugs/Medicinal Chemistry
Antipsychotic Drugs/Medicinal Chemistry
 
Sedative hypnotic drugs /Medicinal Chemistry III(Part Two)
Sedative  hypnotic drugs /Medicinal Chemistry III(Part Two)Sedative  hypnotic drugs /Medicinal Chemistry III(Part Two)
Sedative hypnotic drugs /Medicinal Chemistry III(Part Two)
 
Sedative and hypnotic Drugs/ Medicinal Chemistry III (Part One)
Sedative and hypnotic Drugs/  Medicinal Chemistry III (Part One)Sedative and hypnotic Drugs/  Medicinal Chemistry III (Part One)
Sedative and hypnotic Drugs/ Medicinal Chemistry III (Part One)
 
local anesthetics / Medicinal Chemistry
local anesthetics / Medicinal Chemistry local anesthetics / Medicinal Chemistry
local anesthetics / Medicinal Chemistry
 
General anesthetics / Medicinal Chemistry III
General anesthetics / Medicinal Chemistry IIIGeneral anesthetics / Medicinal Chemistry III
General anesthetics / Medicinal Chemistry III
 

Recently uploaded

Lippincott Microcards_ Microbiology Flash Cards-LWW (2015).pdf
Lippincott Microcards_ Microbiology Flash Cards-LWW (2015).pdfLippincott Microcards_ Microbiology Flash Cards-LWW (2015).pdf
Lippincott Microcards_ Microbiology Flash Cards-LWW (2015).pdfSreeja Cherukuru
 
Measurement of Radiation and Dosimetric Procedure.pptx
Measurement of Radiation and Dosimetric Procedure.pptxMeasurement of Radiation and Dosimetric Procedure.pptx
Measurement of Radiation and Dosimetric Procedure.pptxDr. Dheeraj Kumar
 
CCSC6142 Week 3 Research ethics - Long Hoang.pdf
CCSC6142 Week 3 Research ethics - Long Hoang.pdfCCSC6142 Week 3 Research ethics - Long Hoang.pdf
CCSC6142 Week 3 Research ethics - Long Hoang.pdfMyThaoAiDoan
 
epilepsy and status epilepticus for undergraduate.pptx
epilepsy and status epilepticus  for undergraduate.pptxepilepsy and status epilepticus  for undergraduate.pptx
epilepsy and status epilepticus for undergraduate.pptxMohamed Rizk Khodair
 
LESSON PLAN ON fever.pdf child health nursing
LESSON PLAN ON fever.pdf child health nursingLESSON PLAN ON fever.pdf child health nursing
LESSON PLAN ON fever.pdf child health nursingSakthi Kathiravan
 
SHOCK (Medical SURGICAL BASED EDITION)).pptx
SHOCK (Medical SURGICAL BASED EDITION)).pptxSHOCK (Medical SURGICAL BASED EDITION)).pptx
SHOCK (Medical SURGICAL BASED EDITION)).pptxAbhishek943418
 
Introduction to Sports Injuries by- Dr. Anjali Rai
Introduction to Sports Injuries by- Dr. Anjali RaiIntroduction to Sports Injuries by- Dr. Anjali Rai
Introduction to Sports Injuries by- Dr. Anjali RaiGoogle
 
Study on the Impact of FOCUS-PDCA Management Model on the Disinfection Qualit...
Study on the Impact of FOCUS-PDCA Management Model on the Disinfection Qualit...Study on the Impact of FOCUS-PDCA Management Model on the Disinfection Qualit...
Study on the Impact of FOCUS-PDCA Management Model on the Disinfection Qualit...MehranMouzam
 
Valproic Acid. (VPA). Antiseizure medication
Valproic Acid.  (VPA). Antiseizure medicationValproic Acid.  (VPA). Antiseizure medication
Valproic Acid. (VPA). Antiseizure medicationMohamadAlhes
 
Primary headache and facial pain. (2024)
Primary headache and facial pain. (2024)Primary headache and facial pain. (2024)
Primary headache and facial pain. (2024)Mohamed Rizk Khodair
 
The next social challenge to public health: the information environment.pptx
The next social challenge to public health:  the information environment.pptxThe next social challenge to public health:  the information environment.pptx
The next social challenge to public health: the information environment.pptxTina Purnat
 
Presentation for Bella Mahl 2024-03-28-24-MW-Overview-Bella.pptx
Presentation for Bella Mahl 2024-03-28-24-MW-Overview-Bella.pptxPresentation for Bella Mahl 2024-03-28-24-MW-Overview-Bella.pptx
Presentation for Bella Mahl 2024-03-28-24-MW-Overview-Bella.pptxpdamico1
 
World-Health-Day-2024-My-Health-My-Right.pptx
World-Health-Day-2024-My-Health-My-Right.pptxWorld-Health-Day-2024-My-Health-My-Right.pptx
World-Health-Day-2024-My-Health-My-Right.pptxEx WHO/USAID
 
Big Data Analysis Suggests COVID Vaccination Increases Excess Mortality Of ...
Big Data Analysis Suggests COVID  Vaccination Increases Excess Mortality Of  ...Big Data Analysis Suggests COVID  Vaccination Increases Excess Mortality Of  ...
Big Data Analysis Suggests COVID Vaccination Increases Excess Mortality Of ...sdateam0
 
Music Therapy's Impact in Palliative Care| IAPCON2024| Dr. Tara Rajendran
Music Therapy's Impact in Palliative Care| IAPCON2024| Dr. Tara RajendranMusic Therapy's Impact in Palliative Care| IAPCON2024| Dr. Tara Rajendran
Music Therapy's Impact in Palliative Care| IAPCON2024| Dr. Tara RajendranTara Rajendran
 
Apiculture Chapter 1. Introduction 2.ppt
Apiculture Chapter 1. Introduction 2.pptApiculture Chapter 1. Introduction 2.ppt
Apiculture Chapter 1. Introduction 2.pptkedirjemalharun
 
ANEMIA IN PREGNANCY by Dr. Akebom Kidanemariam
ANEMIA IN PREGNANCY by Dr. Akebom KidanemariamANEMIA IN PREGNANCY by Dr. Akebom Kidanemariam
ANEMIA IN PREGNANCY by Dr. Akebom KidanemariamAkebom Gebremichael
 
Biomechanics- Shoulder Joint!!!!!!!!!!!!
Biomechanics- Shoulder Joint!!!!!!!!!!!!Biomechanics- Shoulder Joint!!!!!!!!!!!!
Biomechanics- Shoulder Joint!!!!!!!!!!!!ibtesaam huma
 
Role of medicinal and aromatic plants in national economy PDF.pdf
Role of medicinal and aromatic plants in national economy PDF.pdfRole of medicinal and aromatic plants in national economy PDF.pdf
Role of medicinal and aromatic plants in national economy PDF.pdfDivya Kanojiya
 
Wessex Health Partners Wessex Integrated Care, Population Health, Research & ...
Wessex Health Partners Wessex Integrated Care, Population Health, Research & ...Wessex Health Partners Wessex Integrated Care, Population Health, Research & ...
Wessex Health Partners Wessex Integrated Care, Population Health, Research & ...Wessex Health Partners
 

Recently uploaded (20)

Lippincott Microcards_ Microbiology Flash Cards-LWW (2015).pdf
Lippincott Microcards_ Microbiology Flash Cards-LWW (2015).pdfLippincott Microcards_ Microbiology Flash Cards-LWW (2015).pdf
Lippincott Microcards_ Microbiology Flash Cards-LWW (2015).pdf
 
Measurement of Radiation and Dosimetric Procedure.pptx
Measurement of Radiation and Dosimetric Procedure.pptxMeasurement of Radiation and Dosimetric Procedure.pptx
Measurement of Radiation and Dosimetric Procedure.pptx
 
CCSC6142 Week 3 Research ethics - Long Hoang.pdf
CCSC6142 Week 3 Research ethics - Long Hoang.pdfCCSC6142 Week 3 Research ethics - Long Hoang.pdf
CCSC6142 Week 3 Research ethics - Long Hoang.pdf
 
epilepsy and status epilepticus for undergraduate.pptx
epilepsy and status epilepticus  for undergraduate.pptxepilepsy and status epilepticus  for undergraduate.pptx
epilepsy and status epilepticus for undergraduate.pptx
 
LESSON PLAN ON fever.pdf child health nursing
LESSON PLAN ON fever.pdf child health nursingLESSON PLAN ON fever.pdf child health nursing
LESSON PLAN ON fever.pdf child health nursing
 
SHOCK (Medical SURGICAL BASED EDITION)).pptx
SHOCK (Medical SURGICAL BASED EDITION)).pptxSHOCK (Medical SURGICAL BASED EDITION)).pptx
SHOCK (Medical SURGICAL BASED EDITION)).pptx
 
Introduction to Sports Injuries by- Dr. Anjali Rai
Introduction to Sports Injuries by- Dr. Anjali RaiIntroduction to Sports Injuries by- Dr. Anjali Rai
Introduction to Sports Injuries by- Dr. Anjali Rai
 
Study on the Impact of FOCUS-PDCA Management Model on the Disinfection Qualit...
Study on the Impact of FOCUS-PDCA Management Model on the Disinfection Qualit...Study on the Impact of FOCUS-PDCA Management Model on the Disinfection Qualit...
Study on the Impact of FOCUS-PDCA Management Model on the Disinfection Qualit...
 
Valproic Acid. (VPA). Antiseizure medication
Valproic Acid.  (VPA). Antiseizure medicationValproic Acid.  (VPA). Antiseizure medication
Valproic Acid. (VPA). Antiseizure medication
 
Primary headache and facial pain. (2024)
Primary headache and facial pain. (2024)Primary headache and facial pain. (2024)
Primary headache and facial pain. (2024)
 
The next social challenge to public health: the information environment.pptx
The next social challenge to public health:  the information environment.pptxThe next social challenge to public health:  the information environment.pptx
The next social challenge to public health: the information environment.pptx
 
Presentation for Bella Mahl 2024-03-28-24-MW-Overview-Bella.pptx
Presentation for Bella Mahl 2024-03-28-24-MW-Overview-Bella.pptxPresentation for Bella Mahl 2024-03-28-24-MW-Overview-Bella.pptx
Presentation for Bella Mahl 2024-03-28-24-MW-Overview-Bella.pptx
 
World-Health-Day-2024-My-Health-My-Right.pptx
World-Health-Day-2024-My-Health-My-Right.pptxWorld-Health-Day-2024-My-Health-My-Right.pptx
World-Health-Day-2024-My-Health-My-Right.pptx
 
Big Data Analysis Suggests COVID Vaccination Increases Excess Mortality Of ...
Big Data Analysis Suggests COVID  Vaccination Increases Excess Mortality Of  ...Big Data Analysis Suggests COVID  Vaccination Increases Excess Mortality Of  ...
Big Data Analysis Suggests COVID Vaccination Increases Excess Mortality Of ...
 
Music Therapy's Impact in Palliative Care| IAPCON2024| Dr. Tara Rajendran
Music Therapy's Impact in Palliative Care| IAPCON2024| Dr. Tara RajendranMusic Therapy's Impact in Palliative Care| IAPCON2024| Dr. Tara Rajendran
Music Therapy's Impact in Palliative Care| IAPCON2024| Dr. Tara Rajendran
 
Apiculture Chapter 1. Introduction 2.ppt
Apiculture Chapter 1. Introduction 2.pptApiculture Chapter 1. Introduction 2.ppt
Apiculture Chapter 1. Introduction 2.ppt
 
ANEMIA IN PREGNANCY by Dr. Akebom Kidanemariam
ANEMIA IN PREGNANCY by Dr. Akebom KidanemariamANEMIA IN PREGNANCY by Dr. Akebom Kidanemariam
ANEMIA IN PREGNANCY by Dr. Akebom Kidanemariam
 
Biomechanics- Shoulder Joint!!!!!!!!!!!!
Biomechanics- Shoulder Joint!!!!!!!!!!!!Biomechanics- Shoulder Joint!!!!!!!!!!!!
Biomechanics- Shoulder Joint!!!!!!!!!!!!
 
Role of medicinal and aromatic plants in national economy PDF.pdf
Role of medicinal and aromatic plants in national economy PDF.pdfRole of medicinal and aromatic plants in national economy PDF.pdf
Role of medicinal and aromatic plants in national economy PDF.pdf
 
Wessex Health Partners Wessex Integrated Care, Population Health, Research & ...
Wessex Health Partners Wessex Integrated Care, Population Health, Research & ...Wessex Health Partners Wessex Integrated Care, Population Health, Research & ...
Wessex Health Partners Wessex Integrated Care, Population Health, Research & ...
 

Anti-Viral Drugs/Medicinal Chemistry

  • 1. ANTI-VIRAL DRUGS Lecture 1 Medicinal Chemistry IV Dr.Narmin Hama Amin University of Sulaimani College of Pharmacy
  • 2. Anti-Viral Drugs ▪ Antiviral agents are substances used in the treatment and prophylaxis of diseases caused by viruses. ▪ Viral diseases include influenza, rabies, yellow fever, poliomyelitis, ornithosis, mumps, measles, ebola, human immuno deficiency virus (HIV), herpes, warts, and small pox
  • 3. What are Viruses? ▪ Viruses are the smallest infectious agents that replicates only inside the living cells of other organisms. ▪ Viruses cannot reproduce on their Own , they use host’s metabolic processes ▪ Range in size from about 20 nm to about 300 nm in diameter ▪ Viruses are lack both a cell wall and cell membrane and they do not carry out metabolic process
  • 5. Structure Of Viruses ➢ The complete structure is known as a virion ▪ Viral particles consist of two to three parts 1. Genetic material , either DNA or RNA 2. Protein coat (Capsid), which surrounds and protects the genetic material 3. Envelope of lipid , lipid layer that surround the protein coat when they are outside cell
  • 6. Classification of Viruses: ▪Herpes viruses to combat diseases such as cold sores, genital herpes ▪ Chicken pox & Shingles ▪ Eye diseases ▪Papillomavirus ▪Hepatitis B virus ▪Mononucleosis RNA viruses: ▪ HIV ( Human immuno deficiency virus) ▪ AIDS ( Acquired immune deficiency syndrome) ▪Hepatitis C ▪ Influenza (or flu) is an airborne, respiratory disease caused by an RNA virus ▪Cold virus ▪Coronavirus DNA Viruses
  • 7. Examples of viruses with diseases
  • 8. Life cycle of the viruses ➢
  • 9. Examples of viral receptors
  • 10.
  • 11. Life cycle of influenza
  • 12. Herpes simplex virus(HSV) structure ▪Herpes simplex viruses -- more commonly known as herpes are categorized into two types: A. Herpes type 1 (HSV-1, or oral herpes) B. Herpes type 2 (HSV-2, or genital herpes)
  • 13. RNA virus (HIV) life cycle ▪ HIV can lead to the development of AIDS. AIDS, or stage 3 HIV, develops when HIV has caused serious damage to the immune system
  • 14. ▪ Diagram of hepatitis B virus (HBV) replication cycle. Attachment to the sodium taurocholate co-transporting polypeptide (NTCP) receptor, and possibly other receptors too, is the initiating event of The sodium taurocholate co-transporting polypeptide (NTCP), a transmembrane protein highly expressed in human hepatocytes that mediates the transport of bile acids, plays a key role in HBV and HDV entry into hepatocytes. ▪ Recently, NTCP has been shown to modulate HCV infection of hepatocytes by regulating innate antiviral immune responses in the liver.
  • 15. ▪ AN EPIDEMIC is a disease that affects a large number of people within a community, population, or region. ▪ A PANDEMIC is an epidemic that’s spread over multiple countries or continents. ➢ For example, when COVID-19 was limited to Wuhan, China, it was an epidemic. The geographical spread turned it into a pandemic. ▪ ENDEMIC is something that belongs to a particular people or country. ▪ AN OUTBREAK is a greater-than-anticipated increase in the number of endemic cases. It can also be a single case in a new area. If it’s not quickly controlled, an outbreak can become an epidemic
  • 16. The major sites for anti-viral drugs
  • 17. Classification of Anti-viral Drugs: 1. Viral attachment and entry are blocked by: A. Maraviroc(HIV) : ▪It is new class of antiretroviral agents , approved as a chemokine receptor CCR5 antagonist in 2007 and is the first anti-HIV agent to act on a molecular target on the host cell rather than the virus ▪Block human immunodeficiency virus type 1 (HIV-1) attachment to the coreceptor and prevents the virus from entering CD4+ cells. ▪It is an example of an agent that works by blocking protein–protein interactions between a viral protein and a host cell protein ▪Maraviroc is a substrate of cytochrome P450 (CYP3A) and p-glycoprotein, and has clinically significant interactions with other drugs including efavirenz and rifampin.
  • 18. B. Enfuvirtide(Fuzeon): ▪Enfuvirtide (INN) is an HIV fusion inhibitor, the first of a class of antiretroviral drugs used in combination therapy for the treatment of HIV-1 infection ▪Exhibits potent and selective inhibition of membrane of viral and cells. ▪ It is a linear 36-amino acid synthetic peptide with the N-terminus acetylated and the C-terminus is a carboxamide. It is composed of naturally occurring L-amino acid residues.
  • 19. 2- Penetration Inhibitors ▪ Interferon α-2B ▪Interferon-mediated inhibition of virus penetration. ▪Interferon is a powerful drug used to treat hepatitis types B, C, and D. It can prevent serious liver damage. It also finds its usefulness in lung carcinoma, breast cancer, multiple myclomas. It is also recommended as a prophylactic agent in cytomegalovirus infection ▪Interferons are proteins that are secreted by the cells when the body is being attacked by a virus like hepatitis B, C, or D. Genetically engineered interferon, given by injection, stops the hepatitis virus from replicating itself and provides a boost to the immune system. ▪ In general, interferons are made up of a mixture of relatively small proteins with molecular weights varying from 20,000 to 1,60,000. These are basically glycoproteins that display specific antiviral properties with species-related characteristics.
  • 20. Pegylated interferon: ▪Pegylated interferon, usually called peginterferon, is a chemically modified form of the standard interferon that treats hepatitis C and rarely hepatitis B. ▪It is also used with ribavirin against hepatitis C infections. ▪The difference between interferon and peginterferon is the PEG, which stands for a molecule called polyethylene glycol. ▪The PEG does nothing to fight the virus, in these formulations, Polyethylene glycol (PEG) is added to make interferon last longer in the body ▪Pegylated interferon is contraindicated in patients with hyperbilirubinaemia.
  • 21. Ribavirin, also known as tribavirin, is an antiviral medication used to treat RSV infection, hepatitis C and some viral hemorrhagic fevers. For hepatitis C, it is used in combination with other medications such as simeprevir, sofosbuvir, peginterferon alfa-2b or peginterferon alfa-2a. Producing a broad-spectrum activity against several RNA and DNA viruses, Ribavirin is a synthetic guanosine nucleoside and antiviral agent that interferes with the synthesis of viral mRNA.
  • 22. 3- Uncoating Inhibitors: Adamantane amines group ▪ They are hydrophobic amines (weak organic bases) with clinical against influenza A ( amantadine and rimantadine) . ▪ Their specificity stems from their ability to bind to block the proton channel formed by the M2 matix protein. The M2 proton channel of the Influenza A virus is the target of the anti-influenza drugs amantadine and rimantadine ▪ Can reduce severity of illness if started within 48 hrs of onset of symptoms.
  • 23. ➢Rimantadine: ▪ Its methyl derivative of amantadine . ▪Interfere with virus uncoating by inhibiting release of specific protein also its more effective and less toxic than amantadine Synthesis of Rimantadine: 1-adamantyl methyl ketoxime 1- acetyladamantane
  • 24. Amantadine , inhibit the uncoating of the viral RNA within the infected host cells thus preventing its replication. ▪ Amantadine is used in the treatment of Parkinson’s disease. It is effective against influenza type-A virus, para influenza, and some RNA virus. It is also used as a dopamine receptor agonist. Synthesis of Amantadine
  • 25. ➢ Tromantadine: ▪ Tromantadine is an antiviral medicine used to treat herpes simplex virus. It is available in a topical gel under trade names Viru-Merz and Viru-Merz Serol. Its performance is similar to acyclovi. ▪ Tromantadine inhibits the early and late events in the virus replication cycle. It changes the glycoproteins of the host cells, therefore impeding the absorption of the virus. It inhibits penetration of the virus. It also prevents uncoating of the virions. Synthesis of Tromantadine (amantadine)
  • 26. 3- Protease inhibitors: ▪Protease inhibitors (PIs) are a class of antiviral drugs that are widely used to treat HIV/AIDS and hepatitis caused by hepatitis C virus. ▪Protease inhibitors prevent viral replication by selectively binding to viral proteases (e.g. HIV-1 protease) and blocking proteolytic cleavage of protein precursors that are necessary for the production of infectious viral particles. ▪HIV-1 protease is a retroviral aspartyl protease, an enzyme involved with peptide bond hydrolysis in retroviruses, that is essential for the life-cycle of HIV, the retrovirus that causes AIDS.
  • 27. A- Saquinavir: was developed by Roche and, as the first PI to reach the market. It has large molecular weight and peptide-like character. ▪It is used to treat HIV infections ▪ It is approximately 98% bound to plasma proteins. ▪Poor oral bioavailability, but is increased with a fatty meal. ▪The drug should be used in combination with at least two other antiretroviral drugs to minimize resistance. B-Indinavir: has better oral bioavailability than saquinavir and is less highly bound to plasma proteins (60%). ▪ When administered with a high-fat diet, indinavir achieves a maximum serum concentration of 77% of the administered dose.
  • 28. C- Nelfinavir: was marketed in 1997 and is used as part of a four-drug combination therapy. Like indinavir and ritonavir, nelfinavir is more potent than saquinavir because of its better pharmacokinetic profile. ▪ Compared with saquinavir, it has a lower molecular weight and log P , and an enhanced aqueous solubility , resulting in enhanced oral bioavailability. D- Atazanavir was approved in June 2003 as the first once daily HIV-1 PI to be used as part of a combination therapy. It is usually administered with ritonavir. E- Lopinavir is a protease inhibitor that has been approved for use in combination with ritonavir for patients with HIV who have not responded to other treatment modalities. ▪ Ritonavir inhibits lopinavir’s metabolism by CYP3A4, causing a higher level of lopinavir in the system.
  • 29. F- Tipranavir. is unique among the PIs because it is not a peptidomimetic compound. It does appear to bind to the active site of HIV-1 protease the same as the peptidomimetics do. ▪ The benefit of this agent is that, because it is a different chemical structure, cross-resistance does not develop to the same extent as seen with the peptidomimetics. ▪ It is used to treat HIV infections that are resistant to other PIs. However, there have been cases of life-threatening liver toxicity ▪ The drug is administered with a booster dose of ritonavir. This protocol inhibits CYP3A4, causing the levels of tipranavir to increase..
  • 30. G - Ritonavir: is an antiretroviral medication used along with other medications to treat HIV/AIDS. This combination treatment is known as highly active antiretroviral therapy (HAART).Often a low dose is used with other protease inhibitors. • It may also be used in combination with other medications for hepatitis C.It is taken by mouth. • Ritonavir ,amprenavir and nelfinavir have similar properties and cautionary statements. All cause dyslipidemia, and they have a host of drug interactions, mainly because they inhibit CYP3A4. These agents must always be used with at least two other antiretroviral agents. Used properly, the PIs are an important part of HIV therapy.
  • 31. 4- Nucleic acid Inhibitors: ▪ These drugs usually act by inhibiting: A. Polymerases B. Reverse Transcriptase ▪They are usually analogues of the purine and pyrimidine bases found in the nucleic acids
  • 32. Purine nucleotides:- a) Acyclovir b) Valacyclovir c) Gancyclovir d) Pencyclovir e) famcyclovir A- Inhibitors of viral DNA polymerase A- Acyclovir ▪ It is a drug of choice in both prophylaxis and treatment of herpes simplex virus, particularly and varicella-zoster(i.e. chickenpox and shingles) significantly. ▪ Herpetic keratitis and herpes genitals are treated effectively by using an ointment containing 5%acyclovir. ▪ Acyclovir has a nucleoside-like structure and contains the same nucleic acid base as deoxyguanosine. However, it lacks the complete sugar ring. ▪ The oral bioavailability of acyclovir is quite low
  • 33. SARs Of Acyclovir 1. Acyclovir is an oxopurine that is guanine substituted by a (2- hydroxyethoxy)methyl substituent at position 9. 2.The length of acyclic side chain attached at N-9 is essential for the anti viral activity. 3.When the acyclic side chain containing hydroxy methylene group was replaced by other substituents,inactive analogues are obtained.This implies that –CH2OH group is essential for anti viral activity. 4.The 9-alkoxy derivative was obtained when a slight modification was brought in the acyl side chain which is highly active against herpes simplex and varicella zoster viruses. 5.Several structural modifications have been brought to acyclovir to obtain high potent drugs. 2-amino-9-(2-hydroxyethoxymethyl)-1H-purin-6-one Acyclovir
  • 34. The effect of acyclovir is the inhibition of viral DNA synthesis. Transport into the cell and monophosphorylation are accomplished by a thymidine kinase that is encoded by the virus itself. The affinity of acyclovir for the viral thymidine kinase is about 200 times that of the corresponding mammalian enzyme.In virally infected cells, it is phosphorylated to form a triphosphate which is the active agent, and so acyclovir is a prodrug . Acyclovir triphosphate prevents DNA replication in two ways: Firstly, it can bind to DNA polymerase and inhibit it. Secondly, the drug acts as a chain terminator
  • 36. ▪ The oral bioavailability of acyclovir is quite low (15– 30%). To overcome this, various prodrugs were developed to increase water solubility. B- Valacyclovir is an l-valyl ester prodrug absorbed from the gut far more effectively than acyclovir. It is a prodrug intended to increase the bioavailability of acyclovir by increasing lipophilicity. The oral bioavailability of valacyclovir is three to five times that of acyclovir
  • 37. Pencyclovir and its prodrug famciclovir are analogues of ganciclovir. ▪ The clinical usefulness of ganciclovir is limited by the toxicity of the drug. Ganciclovir causes myelosuppression, producing neutropenia, thrombocytopenia, and anemia. In famcyclovir, the two alcohol groups of penciclovir are masked as esters making the structure less polar, resulting in better absorption.
  • 38. B- Nucleoside reverse transcriptase inhibitors(NRT I) : ▪ As the enzyme reverse transcriptase is unique to HIV, it serves as an ideal drug target ➢ Zidovudine was developed originally as an anticancer agent but was the first drug to be approved for use in the treatment of AIDS. It is an analogue of deoxythymidine where the sugar 3′-hydroxyl group has been replaced by an azido group ➢lamivudine and emtricitabine: analogues of deoxycytidine where the 3′ carbon has been replaced by sulphur.
  • 39. C-Non-nucleoside reverse transcriptase inhibitors( NNRTI) ➢Nevirapine has a rigid butterfly-like conformation that makes it chiral. ▪ One ‘wing’ interacts through hydrophobic and van der Waals interactions with aromatic residues in the binding site, while the other wing interacts with aliphatic residues. ▪ It is used to treat adults and children with human immunodeficiency virus (HIV) infection. ▪ Nevirapine is more than 90% absorbed by the oral route and is widely distributed throughout the body. It distributes well into breast milk and crosses the placenta
  • 40. 5- Release Inhibitors : Neuraminidase Inhibitors ➢Oseltamivir(Tamiflu) ➢Zanamivir ▪ Drugs use to prevents the Neuraminidase proteins on the surface of IV removing sialic acid from sialic aid-contanining receptors . ▪ Viral budding and downstream replication of IV are inhibited when sialic acid remains on the virion membrane and host cell.
  • 41. Types of influenza or Flu Virus : ▪Type A flu or influenza A viruses are capable of infecting animals, although it is more common for people to suffer the ailments associated with this type of flu. Wild birds commonly act as the hosts for this flu virus. ▪Influenza type B viruses are not classified by subtype and do not cause pandemics. ▪1918 with the death of at least 20 million people worldwide caused by the Spanish flu virus. Epidemics then occurred in 1957 (Asian flu), 1968 (Hong Kong flu), and 1977 (Russian flu).
  • 42. ➢Oseltamivir(Tamiflu) first orally active neuraminidase (NA) inhibitor.a prodrug compound. ➢Active against the influenza A pandemic (H1N1) ➢ Hydrolysis of the ester takes place in the body to give the active carboxylic acid derivative of oseltamivir. ➢As a structural analogue of a key intermediate in sialic acid/NA chemistry, oseltamivir serves as a competitive inhibitor of viral NA by binding strongly to the active site of NA. ➢This interaction ultimately prevents the release of new viral particles from the host cell.
  • 43.
  • 44. ➢Zanamivir ▪ Effective for both influenza A and B. ▪ Poor bioavailability and poor plasma portion binding ▪Use oral inhalation 4-guanidino-2,4-dideoxy-2,3-dehydro-N- acetyl neuraminic aid